Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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9815409 12368 None 21 Mouse Functional pEC50 = 5 5.0 1 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1185481 12368 None 21 Mouse Functional pEC50 = 5 5.0 1 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL416736 12368 None 21 Mouse Functional pEC50 = 5 5.0 1 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
1979 77355 None 47 Mouse Functional pEC50 = 5 5.0 -2089 7
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 10.1021/jm960467d
CHEMBL20835 77355 None 47 Mouse Functional pEC50 = 5 5.0 -2089 7
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 10.1021/jm960467d
2551 794 None 13 Rat Functional pEC50 = 7.0 7.0 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 7.0 7.0 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 7.0 7.0 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 7.0 7.0 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 7.0 7.0 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 7.0 7.0 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 794 None 13 Human Functional pEC50 = 5.0 5.0 -4 13
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
2551.0 794 None 13 Human Functional pEC50 = 5.0 5.0 -4 13
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
298 794 None 13 Human Functional pEC50 = 5.0 5.0 -4 13
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
488 794 None 13 Human Functional pEC50 = 5.0 5.0 -4 13
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
CHEMBL965 794 None 13 Human Functional pEC50 = 5.0 5.0 -4 13
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
DB00411 794 None 13 Human Functional pEC50 = 5.0 5.0 -4 13
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
3652 4097 None 50 Human Functional pEC50 = 7.0 7.0 -109 15
Activation of human cloned muscarinic M3 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M3 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.3c00331
57 4097 None 50 Human Functional pEC50 = 7.0 7.0 -109 15
Activation of human cloned muscarinic M3 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M3 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.3c00331
60809 4097 None 50 Human Functional pEC50 = 7.0 7.0 -109 15
Activation of human cloned muscarinic M3 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M3 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.3c00331
60809.0 4097 None 50 Human Functional pEC50 = 7.0 7.0 -109 15
Activation of human cloned muscarinic M3 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M3 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.3c00331
CHEMBL21536 4097 None 50 Human Functional pEC50 = 7.0 7.0 -109 15
Activation of human cloned muscarinic M3 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M3 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.3c00331
DB15357 4097 None 50 Human Functional pEC50 = 7.0 7.0 -109 15
Activation of human cloned muscarinic M3 receptor expressed in CHO-K1 cells by Calcium flux assay relative to controlActivation of human cloned muscarinic M3 receptor expressed in CHO-K1 cells by Calcium flux assay relative to control
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.3c00331
9838581 11981 None 1 Mouse Functional pEC50 = 6.0 6.0 4 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1183042 11981 None 1 Mouse Functional pEC50 = 6.0 6.0 4 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL277014 11981 None 1 Mouse Functional pEC50 = 6.0 6.0 4 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1 10.1021/jm960467d
3652 4097 None 50 Mouse Functional pEC50 = 5.0 5.0 -1737 15
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
57 4097 None 50 Mouse Functional pEC50 = 5.0 5.0 -1737 15
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
60809 4097 None 50 Mouse Functional pEC50 = 5.0 5.0 -1737 15
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
60809.0 4097 None 50 Mouse Functional pEC50 = 5.0 5.0 -1737 15
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
CHEMBL21536 4097 None 50 Mouse Functional pEC50 = 5.0 5.0 -1737 15
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
DB15357 4097 None 50 Mouse Functional pEC50 = 5.0 5.0 -1737 15
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
10703031 11154 None 0 Mouse Functional pEC50 = 5.0 5.0 - 1
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 196 3 1 6 -0.1 COCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1178347 11154 None 0 Mouse Functional pEC50 = 5.0 5.0 - 1
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 196 3 1 6 -0.1 COCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL22089 11154 None 0 Mouse Functional pEC50 = 5.0 5.0 - 1
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 196 3 1 6 -0.1 COCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
44589681 185394 None 0 Human Functional pEC50 = 7.0 7.0 -12 5
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL485913 185394 None 0 Human Functional pEC50 = 7.0 7.0 -12 5
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
22745278 187169 None 1 Human Functional pEC50 = 7.0 7.0 -53 5
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL491209 187169 None 1 Human Functional pEC50 = 7.0 7.0 -53 5
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
306 3456 None 17 Human Functional pEC50 = 6.9 6.9 -1 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
3536 3456 None 17 Human Functional pEC50 = 6.9 6.9 -1 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
53930639 3456 None 17 Human Functional pEC50 = 6.9 6.9 -1 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
9577995 3456 None 17 Human Functional pEC50 = 6.9 6.9 -1 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
CHEMBL134641 3456 None 17 Human Functional pEC50 = 6.9 6.9 -1 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
3652 4097 None 50 Human Functional pEC50 = 6.9 6.9 -109 15
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57 4097 None 50 Human Functional pEC50 = 6.9 6.9 -109 15
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809 4097 None 50 Human Functional pEC50 = 6.9 6.9 -109 15
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809.0 4097 None 50 Human Functional pEC50 = 6.9 6.9 -109 15
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
CHEMBL21536 4097 None 50 Human Functional pEC50 = 6.9 6.9 -109 15
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
DB15357 4097 None 50 Human Functional pEC50 = 6.9 6.9 -109 15
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
2551 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
1726 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993.0 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
7438 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
CHEMBL978 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
DB06709 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
2230 465 None 43 Mouse Functional pEC50 = 4.9 4.9 -17 9
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
296 465 None 43 Mouse Functional pEC50 = 4.9 4.9 -17 9
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
CHEMBL7303 465 None 43 Mouse Functional pEC50 = 4.9 4.9 -17 9
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
DB04365 465 None 43 Mouse Functional pEC50 = 4.9 4.9 -17 9
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
10375030 13959 None 0 Mouse Functional pEC50 = 4.9 4.9 - 1
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 4 -0.1 C#CCOC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL1196670 13959 None 0 Mouse Functional pEC50 = 4.9 4.9 - 1
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 4 -0.1 C#CCOC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL557795 13959 None 0 Mouse Functional pEC50 = 4.9 4.9 - 1
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 4 -0.1 C#CCOC(=O)C1CCC(N)=NC1 10.1021/jm960467d
2551 794 None 13 Rat Functional pEC50 = 4.9 4.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 4.9 4.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 4.9 4.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 4.9 4.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 4.9 4.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 4.9 4.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
650899 54430 None 6 Human Functional pEC50 = 4.9 4.9 -4 5
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1535797 54430 None 6 Human Functional pEC50 = 4.9 4.9 -4 5
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1609153 54430 None 6 Human Functional pEC50 = 4.9 4.9 -4 5
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
42599070 16085 None 0 Human Functional pEC50 = 6.9 6.9 -316 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223804 16085 None 0 Human Functional pEC50 = 6.9 6.9 -316 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598359 16113 None 0 Human Functional pEC50 = 5.9 5.9 -100 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223864 16113 None 0 Human Functional pEC50 = 5.9 5.9 -100 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
2551 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
9308 17761 None 16 Rat Functional pEC50 = 6.9 6.9 3 9
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL1255785 17761 None 16 Rat Functional pEC50 = 6.9 6.9 3 9
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL12587 17761 None 16 Rat Functional pEC50 = 6.9 6.9 3 9
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL292911 17761 None 16 Rat Functional pEC50 = 6.9 6.9 3 9
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
2551 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 6.9 6.9 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
156015300 177697 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640703 177697 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
10012139 13715 None 8 Mouse Functional pEC50 = 4.9 4.9 2 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL1194965 13715 None 8 Mouse Functional pEC50 = 4.9 4.9 2 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL553602 13715 None 8 Mouse Functional pEC50 = 4.9 4.9 2 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1 10.1021/jm960467d
10240891 208556 None 0 Human Functional pEC50 = 4.8 4.8 -1 3
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 140 1 0 3 0.3 CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL85678 208556 None 0 Human Functional pEC50 = 4.8 4.8 -1 3
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 140 1 0 3 0.3 CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
2551 794 None 13 Rat Functional pEC50 = 6.8 6.8 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 6.8 6.8 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 6.8 6.8 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 6.8 6.8 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 6.8 6.8 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 6.8 6.8 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 794 None 13 Human Functional pEC50 = 4.8 4.8 -4 13
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
2551.0 794 None 13 Human Functional pEC50 = 4.8 4.8 -4 13
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
298 794 None 13 Human Functional pEC50 = 4.8 4.8 -4 13
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
488 794 None 13 Human Functional pEC50 = 4.8 4.8 -4 13
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
CHEMBL965 794 None 13 Human Functional pEC50 = 4.8 4.8 -4 13
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
DB00411 794 None 13 Human Functional pEC50 = 4.8 4.8 -4 13
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
42598360 16111 None 0 Human Functional pEC50 = 5.8 5.8 -630 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223862 16111 None 0 Human Functional pEC50 = 5.8 5.8 -630 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
9990434 106395 None 0 Human Functional pEC50 = 4.8 4.8 -3 3
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 202 2 0 3 0.7 C#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL313918 106395 None 0 Human Functional pEC50 = 4.8 4.8 -3 3
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 202 2 0 3 0.7 C#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
156021744 178219 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4648071 178219 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
92209180 13158 None 4 Mouse Functional pEC50 = 4.8 4.8 2 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
9793884 13158 None 4 Mouse Functional pEC50 = 4.8 4.8 2 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL1190710 13158 None 4 Mouse Functional pEC50 = 4.8 4.8 2 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL541398 13158 None 4 Mouse Functional pEC50 = 4.8 4.8 2 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
124300908 13199 None 3 Mouse Functional pEC50 = 4.8 4.8 1 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
2606 13199 None 3 Mouse Functional pEC50 = 4.8 4.8 1 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL1191029 13199 None 3 Mouse Functional pEC50 = 4.8 4.8 1 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL542065 13199 None 3 Mouse Functional pEC50 = 4.8 4.8 1 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
2551 794 None 13 Human Functional pEC50 = 5.7 5.7 -4 13
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
2551.0 794 None 13 Human Functional pEC50 = 5.7 5.7 -4 13
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
298 794 None 13 Human Functional pEC50 = 5.7 5.7 -4 13
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
488 794 None 13 Human Functional pEC50 = 5.7 5.7 -4 13
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
CHEMBL965 794 None 13 Human Functional pEC50 = 5.7 5.7 -4 13
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
DB00411 794 None 13 Human Functional pEC50 = 5.7 5.7 -4 13
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
156015097 177657 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4640324 177657 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
2551 794 None 13 Rat Functional pEC50 = 6.7 6.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 6.7 6.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 6.7 6.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 6.7 6.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 6.7 6.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 6.7 6.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 794 None 13 Rat Functional pEC50 = 6.7 6.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 6.7 6.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 6.7 6.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 6.7 6.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 6.7 6.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 6.7 6.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
42598829 16087 None 0 Human Functional pEC50 = 5.7 5.7 -251 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223806 16087 None 0 Human Functional pEC50 = 5.7 5.7 -251 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598828 16110 None 0 Human Functional pEC50 = 5.7 5.7 -1584 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223861 16110 None 0 Human Functional pEC50 = 5.7 5.7 -1584 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
187 255 None 24 Human Functional pEC50 = 6.7 6.7 -1 8
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
187.0 255 None 24 Human Functional pEC50 = 6.7 6.7 -1 8
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
294 255 None 24 Human Functional pEC50 = 6.7 6.7 -1 8
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
65 255 None 24 Human Functional pEC50 = 6.7 6.7 -1 8
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
8593 255 None 24 Human Functional pEC50 = 6.7 6.7 -1 8
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
CHEMBL667 255 None 24 Human Functional pEC50 = 6.7 6.7 -1 8
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
DB03128 255 None 24 Human Functional pEC50 = 6.7 6.7 -1 8
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
2551 794 None 13 Rat Functional pEC50 = 7.7 7.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 7.7 7.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 7.7 7.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 7.7 7.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 7.7 7.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 7.7 7.7 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
71737672 2576 None 21 Human Functional pEC50 = 5.7 5.7 -3 6
Activity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2576 None 21 Human Functional pEC50 = 5.7 5.7 -3 6
Activity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2576 None 21 Human Functional pEC50 = 5.7 5.7 -3 6
Activity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
44158142 188777 None 42 Human Functional pEC50 = 5.7 5.7 -1 4
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
CHEMBL503735 188777 None 42 Human Functional pEC50 = 5.7 5.7 -1 4
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
44158142 188777 None 42 Human Functional pEC50 = 5.7 5.7 -1 4
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
CHEMBL503735 188777 None 42 Human Functional pEC50 = 5.7 5.7 -1 4
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
2551 794 None 13 Human Functional pEC50 = 7.6 7.6 -4 13
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
2551.0 794 None 13 Human Functional pEC50 = 7.6 7.6 -4 13
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
298 794 None 13 Human Functional pEC50 = 7.6 7.6 -4 13
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
488 794 None 13 Human Functional pEC50 = 7.6 7.6 -4 13
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
CHEMBL965 794 None 13 Human Functional pEC50 = 7.6 7.6 -4 13
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
DB00411 794 None 13 Human Functional pEC50 = 7.6 7.6 -4 13
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
16071018 16061 None 16 Human Functional pEC50 = 5.6 5.6 -398 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223753 16061 None 16 Human Functional pEC50 = 5.6 5.6 -398 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
42598357 16112 None 0 Human Functional pEC50 = 5.6 5.6 -794 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223863 16112 None 0 Human Functional pEC50 = 5.6 5.6 -794 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
16071018 16061 None 16 Human Functional pEC50 = 5.6 5.6 -398 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
CHEMBL1223753 16061 None 16 Human Functional pEC50 = 5.6 5.6 -398 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
3652 4097 None 50 Human Functional pEC50 = 4.6 4.6 -109 15
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4097 None 50 Human Functional pEC50 = 4.6 4.6 -109 15
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4097 None 50 Human Functional pEC50 = 4.6 4.6 -109 15
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809.0 4097 None 50 Human Functional pEC50 = 4.6 4.6 -109 15
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4097 None 50 Human Functional pEC50 = 4.6 4.6 -109 15
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4097 None 50 Human Functional pEC50 = 4.6 4.6 -109 15
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
71792 78437 None 32 Human Functional pEC50 = 5.6 5.6 -6 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
CHEMBL2111051 78437 None 32 Human Functional pEC50 = 5.6 5.6 -6 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
44251554 7063 None 0 Human Functional pEC50 = 5.6 5.6 -1 4
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory)
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
CHEMBL1084941 7063 None 0 Human Functional pEC50 = 5.6 5.6 -1 4
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory)
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
44422692 11857 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182296 11857 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL228144 11857 None 0 Human Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
14235519 16563 None 3 Mouse Functional pEC50 = 5.6 5.6 4 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 179 1 0 4 1.1 Cc1noc(C2=CCCN(C)C2)n1 10.1021/jm960467d
CHEMBL12378 16563 None 3 Mouse Functional pEC50 = 5.6 5.6 4 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 179 1 0 4 1.1 Cc1noc(C2=CCCN(C)C2)n1 10.1021/jm960467d
187 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
187.0 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
294 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
65 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
8593 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
CHEMBL667 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
DB03128 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
187 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
187.0 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
294 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
65 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
8593 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
CHEMBL667 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
DB03128 255 None 24 Human Functional pEC50 = 8.5 8.5 -1 8
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
9815331 205565 None 1 Rat Functional pEC50 = 8.4 8.4 3 5
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 205565 None 1 Rat Functional pEC50 = 8.4 8.4 3 5
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
9883040 100591 None 0 Human Functional pEC50 = 8.4 8.4 -3 3
In vitro functional agonism against M3 muscarinic receptor (PI)In vitro functional agonism against M3 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL291339 100591 None 0 Human Functional pEC50 = 8.4 8.4 -3 3
In vitro functional agonism against M3 muscarinic receptor (PI)In vitro functional agonism against M3 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL542622 100591 None 0 Human Functional pEC50 = 8.4 8.4 -3 3
In vitro functional agonism against M3 muscarinic receptor (PI)In vitro functional agonism against M3 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
2551 794 None 13 Rat Functional pEC50 = 7.5 7.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 7.5 7.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 7.5 7.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 7.5 7.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 7.5 7.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 7.5 7.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 794 None 13 Rat Functional pEC50 = 6.5 6.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 6.5 6.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 6.5 6.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 6.5 6.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 6.5 6.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 6.5 6.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
71737672 2576 None 21 Rat Functional pEC50 = 5.5 5.5 -5 6
Activity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2576 None 21 Rat Functional pEC50 = 5.5 5.5 -5 6
Activity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2576 None 21 Rat Functional pEC50 = 5.5 5.5 -5 6
Activity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
42599068 16086 None 0 Human Functional pEC50 = 6.5 6.5 -100 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223805 16086 None 0 Human Functional pEC50 = 6.5 6.5 -100 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42599071 16131 None 0 Human Functional pEC50 = 5.5 5.5 -1258 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223939 16131 None 0 Human Functional pEC50 = 5.5 5.5 -1258 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
319 1324 None 32 Human Functional pEC50 = 7.5 7.5 -22 18
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
321 1324 None 32 Human Functional pEC50 = 7.5 7.5 -22 18
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031 1324 None 32 Human Functional pEC50 = 7.5 7.5 -22 18
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031.0 1324 None 32 Human Functional pEC50 = 7.5 7.5 -22 18
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
784 1324 None 32 Human Functional pEC50 = 7.5 7.5 -22 18
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
CHEMBL1346 1324 None 32 Human Functional pEC50 = 7.5 7.5 -22 18
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
DB00496 1324 None 32 Human Functional pEC50 = 7.5 7.5 -22 18
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
2551 794 None 13 Rat Functional pEC50 = 7.5 7.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 7.5 7.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 7.5 7.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 7.5 7.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 7.5 7.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 7.5 7.5 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
42598586 16130 None 0 Human Functional pEC50 = 6.4 6.4 -1 4
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223938 16130 None 0 Human Functional pEC50 = 6.4 6.4 -1 4
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25207745 16133 None 0 Human Functional pEC50 = 5.4 5.4 -398 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223941 16133 None 0 Human Functional pEC50 = 5.4 5.4 -398 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
44253016 80488 None 1 Human Functional pEC50 = 5.4 5.4 -316 4
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
CHEMBL2146597 80488 None 1 Human Functional pEC50 = 5.4 5.4 -316 4
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
16123945 80490 None 10 Human Functional pEC50 = 5.4 5.4 -794 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
CHEMBL2146599 80490 None 10 Human Functional pEC50 = 5.4 5.4 -794 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
156011965 177397 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636528 177397 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
2551 794 None 13 Rat Functional pEC50 = 8.4 8.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 8.4 8.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 8.4 8.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 8.4 8.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 8.4 8.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 8.4 8.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 7.4 7.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
24865895 96058 None 0 Human Functional pEC50 = 6.4 6.4 6 2
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL259662 96058 None 0 Human Functional pEC50 = 6.4 6.4 6 2
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL390842 96058 None 0 Human Functional pEC50 = 6.4 6.4 6 2
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
2551 794 None 13 Rat Functional pEC50 = 6.4 6.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 6.4 6.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 6.4 6.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 6.4 6.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 6.4 6.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 6.4 6.4 2 13
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
319 1324 None 32 Human Functional pEC50 = 7.4 7.4 -22 18
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
321 1324 None 32 Human Functional pEC50 = 7.4 7.4 -22 18
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031 1324 None 32 Human Functional pEC50 = 7.4 7.4 -22 18
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031.0 1324 None 32 Human Functional pEC50 = 7.4 7.4 -22 18
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
784 1324 None 32 Human Functional pEC50 = 7.4 7.4 -22 18
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
CHEMBL1346 1324 None 32 Human Functional pEC50 = 7.4 7.4 -22 18
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
DB00496 1324 None 32 Human Functional pEC50 = 7.4 7.4 -22 18
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
2551 794 None 13 Rat Functional pEC50 = 6.3 6.3 2 13
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
2551.0 794 None 13 Rat Functional pEC50 = 6.3 6.3 2 13
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
298 794 None 13 Rat Functional pEC50 = 6.3 6.3 2 13
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
488 794 None 13 Rat Functional pEC50 = 6.3 6.3 2 13
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
CHEMBL965 794 None 13 Rat Functional pEC50 = 6.3 6.3 2 13
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
DB00411 794 None 13 Rat Functional pEC50 = 6.3 6.3 2 13
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
367 3824 None 10 Human Functional pEC50 = 8.2 8.2 -3 8
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
5487427 3824 None 10 Human Functional pEC50 = 8.2 8.2 -3 8
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
5487427.0 3824 None 10 Human Functional pEC50 = 8.2 8.2 -3 8
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
8592 3824 None 10 Human Functional pEC50 = 8.2 8.2 -3 8
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL1900528 3824 None 10 Human Functional pEC50 = 8.2 8.2 -3 8
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL3305968 3824 None 10 Human Functional pEC50 = 8.2 8.2 -3 8
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL4650755 3824 None 10 Human Functional pEC50 = 8.2 8.2 -3 8
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
DB01409 3824 None 10 Human Functional pEC50 = 8.2 8.2 -3 8
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
10197743 12950 None 5 Mouse Functional pEC50 = 4.3 4.3 - 1
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
92209179 12950 None 5 Mouse Functional pEC50 = 4.3 4.3 - 1
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL1189286 12950 None 5 Mouse Functional pEC50 = 4.3 4.3 - 1
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL538467 12950 None 5 Mouse Functional pEC50 = 4.3 4.3 - 1
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
2551 794 None 13 Human Functional pEC50 = 5.3 5.3 -4 13
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
2551.0 794 None 13 Human Functional pEC50 = 5.3 5.3 -4 13
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 794 None 13 Human Functional pEC50 = 5.3 5.3 -4 13
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 794 None 13 Human Functional pEC50 = 5.3 5.3 -4 13
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 794 None 13 Human Functional pEC50 = 5.3 5.3 -4 13
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 794 None 13 Human Functional pEC50 = 5.3 5.3 -4 13
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
44422699 11855 None 0 Human Functional pEC50 = 4.3 4.3 -1 2
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182272 11855 None 0 Human Functional pEC50 = 4.3 4.3 -1 2
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL227378 11855 None 0 Human Functional pEC50 = 4.3 4.3 -1 2
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
44422692 11857 None 0 Human Functional pEC50 = 4.3 4.3 -1 2
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182296 11857 None 0 Human Functional pEC50 = 4.3 4.3 -1 2
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL228144 11857 None 0 Human Functional pEC50 = 4.3 4.3 -1 2
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
10727260 11992 None 0 Mouse Functional pEC50 = 5.2 5.2 2 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1183133 11992 None 0 Mouse Functional pEC50 = 5.2 5.2 2 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL281411 11992 None 0 Mouse Functional pEC50 = 5.2 5.2 2 2
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
334 236 None 29 Human Functional pEC50 = 5.2 5.2 -144 4
Agonist activity at human muscarinic M3 receptor by calcium mobilization assayAgonist activity at human muscarinic M3 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
9928284 236 None 29 Human Functional pEC50 = 5.2 5.2 -144 4
Agonist activity at human muscarinic M3 receptor by calcium mobilization assayAgonist activity at human muscarinic M3 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
CHEMBL2022960 236 None 29 Human Functional pEC50 = 5.2 5.2 -144 4
Agonist activity at human muscarinic M3 receptor by calcium mobilization assayAgonist activity at human muscarinic M3 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
644390 40425 None 2 Human Functional pEC50 = 4.2 4.2 -2 4
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
CHEMBL1482157 40425 None 2 Human Functional pEC50 = 4.2 4.2 -2 4
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
156014812 178367 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4647437 178367 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650736 178367 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
156009673 178359 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4633816 178359 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650683 178359 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
156015300 177697 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640703 177697 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
42598591 16084 None 0 Human Functional pEC50 = 7.2 7.2 -125 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223803 16084 None 0 Human Functional pEC50 = 7.2 7.2 -125 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25230693 16132 None 0 Human Functional pEC50 = 6.2 6.2 -251 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223940 16132 None 0 Human Functional pEC50 = 6.2 6.2 -251 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
3008304 4023 None 46 Human Functional pEC50 = 5.2 5.2 -1 4
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
7632 4023 None 46 Human Functional pEC50 = 5.2 5.2 -1 4
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
CHEMBL523685 4023 None 46 Human Functional pEC50 = 5.2 5.2 -1 4
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
147230103 180259 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
CHEMBL4748915 180259 None 0 Human Functional pEC50 = 6.2 6.2 -1 2
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
3008304 4023 None 46 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
7632 4023 None 46 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
CHEMBL523685 4023 None 46 Human Functional pEC50 = 5.2 5.2 -1 4
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
3008304 4023 None 46 Human Functional pEC50 = 5.2 5.2 -1 4
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
7632 4023 None 46 Human Functional pEC50 = 5.2 5.2 -1 4
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
CHEMBL523685 4023 None 46 Human Functional pEC50 = 5.2 5.2 -1 4
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
2551 794 None 13 Rat Functional pEC50 = 7.2 7.2 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 7.2 7.2 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 7.2 7.2 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 7.2 7.2 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 7.2 7.2 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 7.2 7.2 2 13
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 794 None 13 Rat Functional pEC50 = 7.2 7.2 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 7.2 7.2 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 7.2 7.2 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 7.2 7.2 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 7.2 7.2 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 7.2 7.2 2 13
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
135409468 2035 None 50 Human Functional pEC50 = 6.2 6.2 -13 5
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
333 2035 None 50 Human Functional pEC50 = 6.2 6.2 -13 5
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
CHEMBL845 2035 None 50 Human Functional pEC50 = 6.2 6.2 -13 5
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
647412 27327 None 5 Human Functional pEC50 = 4.1 4.1 -5 4
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
CHEMBL1367424 27327 None 5 Human Functional pEC50 = 4.1 4.1 -5 4
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
24967746 16062 None 0 Human Functional pEC50 = 7.1 7.1 -199 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223754 16062 None 0 Human Functional pEC50 = 7.1 7.1 -199 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598358 16109 None 0 Human Functional pEC50 = 6.1 6.1 -794 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223860 16109 None 0 Human Functional pEC50 = 6.1 6.1 -794 5
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
10397133 107118 None 1 Human Functional pEC50 = 5.1 5.1 -3 3
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 164 2 0 3 0.3 C#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL315676 107118 None 1 Human Functional pEC50 = 5.1 5.1 -3 3
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 164 2 0 3 0.3 C#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
10397356 120780 None 0 Human Functional pEC50 = 5.1 5.1 -5 3
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL354738 120780 None 0 Human Functional pEC50 = 5.1 5.1 -5 3
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
10130070 120394 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 154 2 0 3 0.7 CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL352908 120394 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 154 2 0 3 0.7 CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
156011965 177397 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636528 177397 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
2551 794 None 13 Rat Functional pEC50 = 7.1 7.1 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551.0 794 None 13 Rat Functional pEC50 = 7.1 7.1 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 794 None 13 Rat Functional pEC50 = 7.1 7.1 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 794 None 13 Rat Functional pEC50 = 7.1 7.1 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 794 None 13 Rat Functional pEC50 = 7.1 7.1 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 794 None 13 Rat Functional pEC50 = 7.1 7.1 2 13
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
10375322 58747 None 0 Human Functional pEC50 = 5.0 5.0 -1 3
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 192 2 0 3 1.1 CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL168545 58747 None 0 Human Functional pEC50 = 5.0 5.0 -1 3
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 192 2 0 3 1.1 CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
2551 794 None 13 Mouse Functional pEC50 = 5 5.0 -93 13
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
2551.0 794 None 13 Mouse Functional pEC50 = 5 5.0 -93 13
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
298 794 None 13 Mouse Functional pEC50 = 5 5.0 -93 13
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
488 794 None 13 Mouse Functional pEC50 = 5 5.0 -93 13
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
CHEMBL965 794 None 13 Mouse Functional pEC50 = 5 5.0 -93 13
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
DB00411 794 None 13 Mouse Functional pEC50 = 5 5.0 -93 13
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
2551 794 None 13 Human Functional pED50 = 7 7.0 -4 13
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
2551.0 794 None 13 Human Functional pED50 = 7 7.0 -4 13
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
298 794 None 13 Human Functional pED50 = 7 7.0 -4 13
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
488 794 None 13 Human Functional pED50 = 7 7.0 -4 13
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
CHEMBL965 794 None 13 Human Functional pED50 = 7 7.0 -4 13
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
DB00411 794 None 13 Human Functional pED50 = 7 7.0 -4 13
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
5487543 208104 None 2 Human Functional pED50 = 5.4 5.4 -41 6
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
CHEMBL81878 208104 None 2 Human Functional pED50 = 5.4 5.4 -41 6
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
9795428 96541 None 4 Human Functional pED50 = 6.1 6.1 -20 5
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
CHEMBL262455 96541 None 4 Human Functional pED50 = 6.1 6.1 -20 5
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
11442478 106534 None 0 Human Functional pIC50 = 9 9.0 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 4 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085073 106534 None 0 Human Functional pIC50 = 9 9.0 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 4 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140113 106534 None 0 Human Functional pIC50 = 9 9.0 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 4 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL5074216 216803 None 0 Rat Functional pIC50 = 9 9.0 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@@H]3CCN(C)C3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5074599 216807 None 2 Rat Functional pIC50 = 9 9.0 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5074216 216803 None 0 Rat Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@@H]3CCN(C)C3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5086393 217515 None 0 Rat Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44589585 189000 None 0 Human Functional pIC50 = 8.7 8.7 1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 10 4 5 4.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL507375 189000 None 0 Human Functional pIC50 = 8.7 8.7 1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 10 4 5 4.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555474 189000 None 0 Human Functional pIC50 = 8.7 8.7 1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 10 4 5 4.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5074599 216807 None 2 Rat Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44232700 106567 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3084399 106567 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3140218 106567 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
11341753 187409 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 8 2 4 4.1 CCOc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492978 187409 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 8 2 4 4.1 CCOc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11341940 187468 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 CC1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493328 187468 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 CC1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
11364721 192833 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 427 7 2 4 3.9 CC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL522020 192833 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 427 7 2 4 3.9 CC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44589495 186086 None 0 Human Functional pIC50 = 8 8.0 10 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 5 7 3.8 CCCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL486982 186086 None 0 Human Functional pIC50 = 8 8.0 10 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 5 7 3.8 CCCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590173 189200 None 0 Human Functional pIC50 = 8 8.0 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL510029 189200 None 0 Human Functional pIC50 = 8 8.0 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555019 189200 None 0 Human Functional pIC50 = 8 8.0 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5076886 216955 None 0 Rat Functional pIC50 = 8 8.0 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3C[C@H]4CC[C@H](C3)N4C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
71452454 83952 None 0 Human Functional pIC50 = 8.0 8.0 41 2
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 603 9 3 7 3.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206587 83952 None 0 Human Functional pIC50 = 8.0 8.0 41 2
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 603 9 3 7 3.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2012.09.085
11552174 103556 None 0 Human Functional pIC50 = 8.0 8.0 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085090 103556 None 0 Human Functional pIC50 = 8.0 8.0 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
11330061 187418 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492997 187418 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2009.01.098
44589570 172860 None 0 Human Functional pIC50 = 7 7.0 15 2
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 10 5 6 3.5 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL451040 172860 None 0 Human Functional pIC50 = 7 7.0 15 2
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 10 5 6 3.5 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589498 172861 None 0 Human Functional pIC50 = 7 7.0 3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 572 11 5 7 3.8 O=C(Nc1ccc(C(=O)OCC2CC2)cc1)N[C@@H](Cc1ccc(O)cc1)C(=O)NC1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL451043 172861 None 0 Human Functional pIC50 = 7 7.0 3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 572 11 5 7 3.8 O=C(Nc1ccc(C(=O)OCC2CC2)cc1)N[C@@H](Cc1ccc(O)cc1)C(=O)NC1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.09.020
44573500 187826 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1Cl 10.1016/j.bmcl.2009.01.098
CHEMBL495361 187826 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1Cl 10.1016/j.bmcl.2009.01.098
44589575 175747 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 596 9 4 7 2.9 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)N4CCOCC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL458105 175747 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 596 9 4 7 2.9 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)N4CCOCC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
145955917 162578 None 0 Human Functional pIC50 = 5 5.0 -29 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 418 6 2 4 4.2 NC[C@H]1CC[C@H](CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
CHEMBL4167221 162578 None 0 Human Functional pIC50 = 5 5.0 -29 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 418 6 2 4 4.2 NC[C@H]1CC[C@H](CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
44233187 86059 None 0 Human Functional pIC50 = 6.0 6.0 -2 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2306159 86059 None 0 Human Functional pIC50 = 6.0 6.0 -2 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233187 86059 None 0 Human Functional pIC50 = 6.0 6.0 -2 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2306159 86059 None 0 Human Functional pIC50 = 6.0 6.0 -2 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
76324336 103552 None 0 Human Functional pIC50 = 7.0 7.0 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085086 103552 None 0 Human Functional pIC50 = 7.0 7.0 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
76331543 103558 None 0 Human Functional pIC50 = 7.0 7.0 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 4 4.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085092 103558 None 0 Human Functional pIC50 = 7.0 7.0 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 4 4.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
57758637 106555 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 441 7 0 1 7.2 C[N+]1(CCC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084466 106555 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 441 7 0 1 7.2 C[N+]1(CCC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140183 106555 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 441 7 0 1 7.2 C[N+]1(CCC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44232702 106559 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3084401 106559 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3140203 106559 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
11547053 106521 None 0 Human Functional pIC50 = 8.0 8.0 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 3 5.0 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085074 106521 None 0 Human Functional pIC50 = 8.0 8.0 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 3 5.0 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140097 106521 None 0 Human Functional pIC50 = 8.0 8.0 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 3 5.0 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
145958296 162376 None 0 Human Functional pIC50 = 6.0 6.0 -38 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4164075 162376 None 0 Human Functional pIC50 = 6.0 6.0 -38 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
142416754 162436 None 0 Human Functional pIC50 = 5.0 5.0 -112 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 480 8 2 4 5.2 FC1(F)CCC(NC/C=C\CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
CHEMBL4164874 162436 None 0 Human Functional pIC50 = 5.0 5.0 -112 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 480 8 2 4 5.2 FC1(F)CCC(NC/C=C\CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
44232708 106542 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cc(F)cc(F)c1)c1cc(F)cc(F)c1)C2 10.1021/jm900736e
CHEMBL3084407 106542 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cc(F)cc(F)c1)c1cc(F)cc(F)c1)C2 10.1021/jm900736e
CHEMBL3140145 106542 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cc(F)cc(F)c1)c1cc(F)cc(F)c1)C2 10.1021/jm900736e
76320693 103548 None 0 Human Functional pIC50 = 5.9 5.9 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085082 103548 None 0 Human Functional pIC50 = 5.9 5.9 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
76309756 103549 None 0 Human Functional pIC50 = 5.9 5.9 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 375 4 0 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085083 103549 None 0 Human Functional pIC50 = 5.9 5.9 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 375 4 0 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44590174 170160 None 0 Human Functional pIC50 = 7.9 7.9 -3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 651 10 3 6 4.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Br)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL444300 170160 None 0 Human Functional pIC50 = 7.9 7.9 -3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 651 10 3 6 4.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Br)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL466271 170160 None 0 Human Functional pIC50 = 7.9 7.9 -3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 651 10 3 6 4.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Br)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590177 189030 None 0 Human Functional pIC50 = 7.9 7.9 -5 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 677 12 3 7 5.1 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(=O)c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL507874 189030 None 0 Human Functional pIC50 = 7.9 7.9 -5 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 677 12 3 7 5.1 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(=O)c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL554918 189030 None 0 Human Functional pIC50 = 7.9 7.9 -5 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 677 12 3 7 5.1 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(=O)c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5076535 216933 None 0 Rat Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCCN(C)C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
11699452 12625 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 456 8 1 2 5.8 Cc1ccc(C(O)(c2ccc(C)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1187080 12625 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 456 8 1 2 5.8 Cc1ccc(C(O)(c2ccc(C)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL489626 12625 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 456 8 1 2 5.8 Cc1ccc(C(O)(c2ccc(C)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
44590179 172820 None 0 Human Functional pIC50 = 6.9 6.9 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccccc2Cl)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450538 172820 None 0 Human Functional pIC50 = 6.9 6.9 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccccc2Cl)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL553446 172820 None 0 Human Functional pIC50 = 6.9 6.9 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccccc2Cl)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44573621 187318 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 477 8 2 4 5.5 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492391 187318 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 477 8 2 4 5.5 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2009.01.098
44573263 193259 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CN2CCNCC2)cc1-c1cccc(CNC(=O)c2ccc3c(c2)OCO3)c1 10.1016/j.bmcl.2009.01.098
CHEMBL522992 193259 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CN2CCNCC2)cc1-c1cccc(CNC(=O)c2ccc3c(c2)OCO3)c1 10.1016/j.bmcl.2009.01.098
44590181 173668 None 0 Human Functional pIC50 = 5.9 5.9 -25 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 633 12 3 8 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)c(OC)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL453248 173668 None 0 Human Functional pIC50 = 5.9 5.9 -25 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 633 12 3 8 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)c(OC)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL551113 173668 None 0 Human Functional pIC50 = 5.9 5.9 -25 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 633 12 3 8 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)c(OC)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
162646559 179746 None 0 Human Functional pIC50 = 5.9 5.9 -97 4
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@@H](C)C1 10.1021/acsmedchemlett.0c00626
CHEMBL4742997 179746 None 0 Human Functional pIC50 = 5.9 5.9 -97 4
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@@H](C)C1 10.1021/acsmedchemlett.0c00626
71459724 84041 None 0 Human Functional pIC50 = 7.9 7.9 63 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2207177 84041 None 0 Human Functional pIC50 = 7.9 7.9 63 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
42626092 12639 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187132 12639 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL491246 12639 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
145956824 162355 None 0 Human Functional pIC50 = 4.9 4.9 -1412 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.1 NCC1CC1CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4163770 162355 None 0 Human Functional pIC50 = 4.9 4.9 -1412 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.1 NCC1CC1CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
44233417 86080 None 0 Human Functional pIC50 = 5.9 5.9 -1 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2307674 86080 None 0 Human Functional pIC50 = 5.9 5.9 -1 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233417 86080 None 0 Human Functional pIC50 = 5.9 5.9 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2307674 86080 None 0 Human Functional pIC50 = 5.9 5.9 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
76324303 103304 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.6 CN1[C@H]2CC[C@@H]1C[C@H](CCC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084394 103304 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.6 CN1[C@H]2CC[C@@H]1C[C@H](CCC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
76327870 103307 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 273 4 1 2 3.5 CCC(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1021/jm900736e
CHEMBL3084397 103307 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 273 4 1 2 3.5 CCC(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1021/jm900736e
76327903 103559 None 0 Human Functional pIC50 = 6.9 6.9 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 381 4 0 5 4.4 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085093 103559 None 0 Human Functional pIC50 = 6.9 6.9 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 381 4 0 5 4.4 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
76316969 106579 None 0 Human Functional pIC50 = 6.9 6.9 -2 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 396 4 0 4 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(C#N)c1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085075 106579 None 0 Human Functional pIC50 = 6.9 6.9 -2 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 396 4 0 4 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(C#N)c1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140262 106579 None 0 Human Functional pIC50 = 6.9 6.9 -2 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 396 4 0 4 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(C#N)c1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
71455969 83964 None 0 Human Functional pIC50 = 6.9 6.9 3 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 581 12 4 5 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206603 83964 None 0 Human Functional pIC50 = 6.9 6.9 3 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 581 12 4 5 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
1765112 103303 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 307 3 1 2 3.8 CN1[C@H]2CC[C@@H]1C[C@H](C(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084393 103303 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 307 3 1 2 3.8 CN1[C@H]2CC[C@@H]1C[C@H](C(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
25034111 193527 None 0 Human Functional pIC50 = 7.8 7.8 7 3
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL526009 193527 None 0 Human Functional pIC50 = 7.8 7.8 7 3
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
16040727 169546 None 0 Human Functional pIC50 = 7.8 7.8 -3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 649 11 3 6 5.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL442672 169546 None 0 Human Functional pIC50 = 7.8 7.8 -3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 649 11 3 6 5.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL495102 169546 None 0 Human Functional pIC50 = 7.8 7.8 -3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 649 11 3 6 5.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590124 169897 None 0 Human Functional pIC50 = 7.8 7.8 39 2
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 4 6 4.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL443925 169897 None 0 Human Functional pIC50 = 7.8 7.8 39 2
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 4 6 4.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590172 170421 None 0 Human Functional pIC50 = 7.8 7.8 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 591 10 3 6 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL444688 170421 None 0 Human Functional pIC50 = 7.8 7.8 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 591 10 3 6 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL527216 170421 None 0 Human Functional pIC50 = 7.8 7.8 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 591 10 3 6 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590171 178853 None 0 Human Functional pIC50 = 7.8 7.8 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 587 10 3 6 4.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL468609 178853 None 0 Human Functional pIC50 = 7.8 7.8 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 587 10 3 6 4.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL554632 178853 None 0 Human Functional pIC50 = 7.8 7.8 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 587 10 3 6 4.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590125 183967 None 0 Human Functional pIC50 = 7.8 7.8 12 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 530 10 4 6 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL480878 183967 None 0 Human Functional pIC50 = 7.8 7.8 12 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 530 10 4 6 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590170 188478 None 0 Human Functional pIC50 = 7.8 7.8 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 4 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL501348 188478 None 0 Human Functional pIC50 = 7.8 7.8 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 4 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL553431 188478 None 0 Human Functional pIC50 = 7.8 7.8 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 4 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
25034111 193527 None 0 Human Functional pIC50 = 7.8 7.8 7 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL526009 193527 None 0 Human Functional pIC50 = 7.8 7.8 7 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
76309754 106577 None 0 Human Functional pIC50 = 6.8 6.8 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085062 106577 None 0 Human Functional pIC50 = 6.8 6.8 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
CHEMBL3140260 106577 None 0 Human Functional pIC50 = 6.8 6.8 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
44589571 172690 None 0 Human Functional pIC50 = 6.8 6.8 10 2
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 580 11 5 6 3.5 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCC4CC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL448904 172690 None 0 Human Functional pIC50 = 6.8 6.8 10 2
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 580 11 5 6 3.5 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCC4CC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
71452456 83970 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 525 10 4 5 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(C)CCCCCC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206609 83970 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 525 10 4 5 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(C)CCCCCC2)cc1 10.1016/j.bmcl.2012.09.085
25034180 188519 None 0 Human Functional pIC50 = 5.8 5.8 -1 3
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL502000 188519 None 0 Human Functional pIC50 = 5.8 5.8 -1 3
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
44573744 187755 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 7 1 5 4.2 CCN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL494996 187755 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 7 1 5 4.2 CCN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44589573 189013 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 616 11 5 6 4.3 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL507581 189013 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 616 11 5 6 4.3 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
11510358 106540 None 0 Human Functional pIC50 = 7.8 7.8 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 355 4 0 3 4.2 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085069 106540 None 0 Human Functional pIC50 = 7.8 7.8 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 355 4 0 3 4.2 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140143 106540 None 0 Human Functional pIC50 = 7.8 7.8 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 355 4 0 3 4.2 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44232947 106525 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccsc1)c1ccsc1)C2 10.1021/jm900736e
CHEMBL3084411 106525 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccsc1)c1ccsc1)C2 10.1021/jm900736e
CHEMBL3140100 106525 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccsc1)c1ccsc1)C2 10.1021/jm900736e
11664153 12761 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1cccc(C(O)(c2cccc(OC)c2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL1187845 12761 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1cccc(C(O)(c2cccc(OC)c2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL523767 12761 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1cccc(C(O)(c2cccc(OC)c2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
76324304 103305 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 322 4 1 3 3.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccn1)C2 10.1021/jm900736e
CHEMBL3084395 103305 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 322 4 1 3 3.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccn1)C2 10.1021/jm900736e
15945874 188873 None 0 Human Functional pIC50 = 7.7 7.7 7 3
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL505452 188873 None 0 Human Functional pIC50 = 7.7 7.7 7 3
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
44573578 187313 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 7 2 5 3.5 COC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492374 187313 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 7 2 5 3.5 COC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11455956 187707 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 463 7 2 5 3.1 CS(=O)(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494749 187707 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 463 7 2 5 3.1 CS(=O)(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44590033 183784 None 0 Human Functional pIC50 = 7.7 7.7 12 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL480299 183784 None 0 Human Functional pIC50 = 7.7 7.7 12 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
15945874 188873 None 0 Human Functional pIC50 = 7.7 7.7 7 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL505452 188873 None 0 Human Functional pIC50 = 7.7 7.7 7 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589984 190667 None 0 Human Functional pIC50 = 7.7 7.7 7 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL518001 190667 None 0 Human Functional pIC50 = 7.7 7.7 7 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
1201549 597 None 17 Human Functional pIC50 = 7.7 7.7 -4 26
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
1201549.0 597 None 17 Human Functional pIC50 = 7.7 7.7 -4 26
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
333 597 None 17 Human Functional pIC50 = 7.7 7.7 -4 26
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
7601 597 None 17 Human Functional pIC50 = 7.7 7.7 -4 26
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
CHEMBL1201203 597 None 17 Human Functional pIC50 = 7.7 7.7 -4 26
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
CHEMBL438151 597 None 17 Human Functional pIC50 = 7.7 7.7 -4 26
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
DB00245 597 None 17 Human Functional pIC50 = 7.7 7.7 -4 26
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
CHEMBL5076445 216929 None 0 Rat Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CCN3C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5078006 217016 None 0 Rat Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5086393 217515 None 0 Rat Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44232953 103446 None 0 Human Functional pIC50 = 5.7 5.7 -1 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
CHEMBL3084663 103446 None 0 Human Functional pIC50 = 5.7 5.7 -1 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
44232953 103446 None 0 Human Functional pIC50 = 5.7 5.7 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
CHEMBL3084663 103446 None 0 Human Functional pIC50 = 5.7 5.7 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
71459689 83950 None 0 Human Functional pIC50 = 6.7 6.7 -1 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 595 13 4 5 5.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206585 83950 None 0 Human Functional pIC50 = 6.7 6.7 -1 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 595 13 4 5 5.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
44573264 187308 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2ccc(F)c(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL492359 187308 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2ccc(F)c(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44573619 187708 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 7 3 4 3.6 CC(=O)Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494752 187708 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 7 3 4 3.6 CC(=O)Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11714747 187739 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 7 2 4 3.8 CN(C)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494950 187739 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 7 2 4 3.8 CN(C)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11578568 187740 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 400 6 3 4 3.3 Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494951 187740 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 400 6 3 4 3.3 Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44573661 188488 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 401 6 3 4 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(O)c1 10.1016/j.bmcl.2009.01.098
CHEMBL501486 188488 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 401 6 3 4 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(O)c1 10.1016/j.bmcl.2009.01.098
25034112 188500 None 0 Human Functional pIC50 = 4.7 4.7 -1 3
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL501727 188500 None 0 Human Functional pIC50 = 4.7 4.7 -1 3
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
11690968 106557 None 0 Human Functional pIC50 = 8.7 8.7 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085072 106557 None 0 Human Functional pIC50 = 8.7 8.7 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140185 106557 None 0 Human Functional pIC50 = 8.7 8.7 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
11518068 106562 None 0 Human Functional pIC50 = 8.6 8.6 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085059 106562 None 0 Human Functional pIC50 = 8.6 8.6 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140213 106562 None 0 Human Functional pIC50 = 8.6 8.6 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
11583262 106553 None 0 Human Functional pIC50 = 8.6 8.6 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085060 106553 None 0 Human Functional pIC50 = 8.6 8.6 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140181 106553 None 0 Human Functional pIC50 = 8.6 8.6 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
69444105 103542 None 0 Human Functional pIC50 = 7.7 7.7 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085077 103542 None 0 Human Functional pIC50 = 7.7 7.7 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44233675 103433 None 0 Human Functional pIC50 = 6.7 6.7 -1 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084639 103433 None 0 Human Functional pIC50 = 6.7 6.7 -1 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233675 103433 None 0 Human Functional pIC50 = 6.7 6.7 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084639 103433 None 0 Human Functional pIC50 = 6.7 6.7 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
11712408 106578 None 0 Human Functional pIC50 = 7.7 7.7 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
CHEMBL3085067 106578 None 0 Human Functional pIC50 = 7.7 7.7 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
CHEMBL3140261 106578 None 0 Human Functional pIC50 = 7.7 7.7 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
76327901 103550 None 0 Human Functional pIC50 = 5.7 5.7 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 380 5 0 4 4.5 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
CHEMBL3085084 103550 None 0 Human Functional pIC50 = 5.7 5.7 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 380 5 0 4 4.5 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
11508710 103555 None 0 Human Functional pIC50 = 7.6 7.6 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085089 103555 None 0 Human Functional pIC50 = 7.6 7.6 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
42626088 12628 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
CHEMBL1187091 12628 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
CHEMBL490236 12628 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
71450615 83965 None 0 Human Functional pIC50 = 6.7 6.7 1 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 609 14 4 5 5.5 CC[N+](CC)(CCNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)Nc1ccc(C(=O)OC(C)C)cc1)Cc1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206604 83965 None 0 Human Functional pIC50 = 6.7 6.7 1 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 609 14 4 5 5.5 CC[N+](CC)(CCNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)Nc1ccc(C(=O)OC(C)C)cc1)Cc1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.085
44232951 106526 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 378 4 1 1 5.3 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CCC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3084416 106526 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 378 4 1 1 5.3 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CCC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3140101 106526 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 378 4 1 1 5.3 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CCC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
10092649 193182 None 43 Human Functional pIC50 = 5.6 5.6 -29 11
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 193182 None 43 Human Functional pIC50 = 5.6 5.6 -29 11
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
145954567 162601 None 0 Human Functional pIC50 = 4.6 4.6 -100 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 416 6 2 4 4.3 NCC1=C(CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CCCC1 10.1021/acsmedchemlett.7b00406
CHEMBL4167521 162601 None 0 Human Functional pIC50 = 4.6 4.6 -100 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 416 6 2 4 4.3 NCC1=C(CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CCCC1 10.1021/acsmedchemlett.7b00406
76324335 103547 None 0 Human Functional pIC50 = 5.6 5.6 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085081 103547 None 0 Human Functional pIC50 = 5.6 5.6 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
10092649 193182 None 43 Human Functional pIC50 = 5.6 5.6 -29 11
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 193182 None 43 Human Functional pIC50 = 5.6 5.6 -29 11
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
71450617 83971 None 0 Human Functional pIC50 = 6.6 6.6 1 2
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 527 12 4 5 4.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206610 83971 None 0 Human Functional pIC50 = 6.6 6.6 1 2
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 527 12 4 5 4.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2012.09.085
44455159 97818 None 0 Rat Functional pIC50 = 4.6 4.6 -20 5
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 383 5 1 3 4.2 CCN1CCN(c2ccc(NC(=O)[C@H]3C[C@@H]3c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL271704 97818 None 0 Rat Functional pIC50 = 4.6 4.6 -20 5
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 383 5 1 3 4.2 CCN1CCN(c2ccc(NC(=O)[C@H]3C[C@@H]3c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
44234432 106541 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(Cl)c1)c1cccc(Cl)c1)C2 10.1021/jm900736e
CHEMBL3084402 106541 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(Cl)c1)c1cccc(Cl)c1)C2 10.1021/jm900736e
CHEMBL3140144 106541 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(Cl)c1)c1cccc(Cl)c1)C2 10.1021/jm900736e
44590180 172749 None 0 Human Functional pIC50 = 7.6 7.6 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 5.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL449640 172749 None 0 Human Functional pIC50 = 7.6 7.6 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 5.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540398 172749 None 0 Human Functional pIC50 = 7.6 7.6 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 5.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590167 179130 None 0 Human Functional pIC50 = 7.6 7.6 3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 494 10 4 6 2.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL471214 179130 None 0 Human Functional pIC50 = 7.6 7.6 3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 494 10 4 6 2.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590182 183257 None 0 Human Functional pIC50 = 7.6 7.6 12 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 532 9 5 7 3.0 COC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL479526 183257 None 0 Human Functional pIC50 = 7.6 7.6 12 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 532 9 5 7 3.0 COC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590034 190086 None 0 Human Functional pIC50 = 7.6 7.6 12 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(OC)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL517087 190086 None 0 Human Functional pIC50 = 7.6 7.6 12 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(OC)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
44573370 187554 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cc(-c2cccc(CN3CCNCC3)c2)ccc1F)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL493939 187554 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cc(-c2cccc(CN3CCNCC3)c2)ccc1F)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44573662 187633 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 399 6 2 3 4.0 Cc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494410 187633 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 399 6 2 3 4.0 Cc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44573420 187715 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 465 7 2 6 3.0 O=S(=O)(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494778 187715 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 465 7 2 6 3.0 O=S(=O)(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44589497 175397 None 0 Human Functional pIC50 = 6.6 6.6 5 2
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 574 11 5 7 4.0 CC(C)COC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL457302 175397 None 0 Human Functional pIC50 = 6.6 6.6 5 2
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 574 11 5 7 4.0 CC(C)COC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
11285415 187307 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 458 6 1 4 3.9 C[N+]1(C)CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL492358 187307 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 458 6 1 4 3.9 C[N+]1(C)CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL538863 187307 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 458 6 1 4 3.9 C[N+]1(C)CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44573372 193399 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1F)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL524031 193399 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1F)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44589499 191950 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 540 9 5 6 2.7 CNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL519893 191950 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 540 9 5 6 2.7 CNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
11442669 74305 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2023761 74305 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
76320694 103551 None 0 Human Functional pIC50 = 6.6 6.6 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
CHEMBL3085085 103551 None 0 Human Functional pIC50 = 6.6 6.6 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
11617374 103543 None 0 Human Functional pIC50 = 7.6 7.6 2 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085078 103543 None 0 Human Functional pIC50 = 7.6 7.6 2 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
71455965 83954 None 0 Human Functional pIC50 = 7.6 7.6 3 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](Cc3ccc(Cl)cc3)(C(C)C)CC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206589 83954 None 0 Human Functional pIC50 = 7.6 7.6 3 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](Cc3ccc(Cl)cc3)(C(C)C)CC2)cc1 10.1016/j.bmcl.2012.09.085
44234194 103451 None 0 Human Functional pIC50 = 5.6 5.6 -1 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 412 7 1 3 3.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(C)(=O)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084670 103451 None 0 Human Functional pIC50 = 5.6 5.6 -1 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 412 7 1 3 3.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(C)(=O)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44234194 103451 None 0 Human Functional pIC50 = 5.6 5.6 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 412 7 1 3 3.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(C)(=O)=O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084670 103451 None 0 Human Functional pIC50 = 5.6 5.6 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 412 7 1 3 3.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(C)(=O)=O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
9044803 124172 None 12 Human Functional pIC50 = 4.6 4.6 -1 2
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633650 124172 None 12 Human Functional pIC50 = 4.6 4.6 -1 2
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
9044803 124172 None 12 Human Functional pIC50 = 4.6 4.6 -1 2
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633650 124172 None 12 Human Functional pIC50 = 4.6 4.6 -1 2
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
44233419 103454 None 0 Human Functional pIC50 = 5.5 5.5 -1 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 6 1 2 4.4 CC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
CHEMBL3084674 103454 None 0 Human Functional pIC50 = 5.5 5.5 -1 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 6 1 2 4.4 CC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
44233419 103454 None 0 Human Functional pIC50 = 5.5 5.5 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 6 1 2 4.4 CC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
CHEMBL3084674 103454 None 0 Human Functional pIC50 = 5.5 5.5 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 6 1 2 4.4 CC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
44232710 106550 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(F)c(F)c1)c1ccc(F)c(F)c1)C2 10.1021/jm900736e
CHEMBL3084408 106550 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(F)c(F)c1)c1ccc(F)c(F)c1)C2 10.1021/jm900736e
CHEMBL3140173 106550 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(F)c(F)c1)c1ccc(F)c(F)c1)C2 10.1021/jm900736e
11503336 106570 None 0 Human Functional pIC50 = 8.5 8.5 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085071 106570 None 0 Human Functional pIC50 = 8.5 8.5 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140242 106570 None 0 Human Functional pIC50 = 8.5 8.5 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL5078006 217016 None 0 Rat Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
11557048 187759 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 497 8 2 5 3.4 CN1CCN(Cc2cccc(C(=O)NCc3cccc(-c4cccc(CN5CCNCC5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL495028 187759 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 497 8 2 5 3.4 CN1CCN(Cc2cccc(C(=O)NCc3cccc(-c4cccc(CN5CCNCC5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
11633399 12623 None 0 Human Functional pIC50 = 4.5 4.5 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 352 6 1 2 3.6 COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187077 12623 None 0 Human Functional pIC50 = 4.5 4.5 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 352 6 1 2 3.6 COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL489225 12623 None 0 Human Functional pIC50 = 4.5 4.5 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 352 6 1 2 3.6 COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
11318734 187436 None 0 Human Functional pIC50 = 7.5 7.5 5 2
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 6 2 5 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL493079 187436 None 0 Human Functional pIC50 = 7.5 7.5 5 2
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 6 2 5 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
11273131 193238 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)OCO3)cc1-c1cccc(CN2CCNCC2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL522838 193238 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)OCO3)cc1-c1cccc(CN2CCNCC2)c1 10.1016/j.bmcl.2009.01.098
44590036 188484 None 0 Human Functional pIC50 = 7.5 7.5 6 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 574 10 4 8 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL501419 188484 None 0 Human Functional pIC50 = 7.5 7.5 6 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 574 10 4 8 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590176 189174 None 0 Human Functional pIC50 = 7.5 7.5 -3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 4.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(F)(F)F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL509614 189174 None 0 Human Functional pIC50 = 7.5 7.5 -3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 4.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(F)(F)F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555707 189174 None 0 Human Functional pIC50 = 7.5 7.5 -3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 4.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(F)(F)F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
24882532 95170 None 0 Rat Functional pIC50 = 5.5 5.5 -7 4
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL255523 95170 None 0 Rat Functional pIC50 = 5.5 5.5 -7 4
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
44573265 187371 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(-c2cccc(CNC(=O)c3ccc4c(c3)OCO4)c2)cc1CN1CCNCC1 10.1016/j.bmcl.2009.01.098
CHEMBL492756 187371 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(-c2cccc(CNC(=O)c3ccc4c(c3)OCO4)c2)cc1CN1CCNCC1 10.1016/j.bmcl.2009.01.098
44573501 187419 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.01.098
CHEMBL492998 187419 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.01.098
44573663 187634 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 413 7 2 3 4.3 CCc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494411 187634 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 413 7 2 3 4.3 CCc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11421571 187723 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 O=C(NCc1cccc(-c2cccc(CN3CCCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494836 187723 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 O=C(NCc1cccc(-c2cccc(CN3CCCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44573423 187758 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1ccccc1C(=O)NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL495025 187758 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1ccccc1C(=O)NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1 10.1016/j.bmcl.2009.01.098
44589529 186626 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 554 10 5 6 3.1 CCNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL487764 186626 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 554 10 5 6 3.1 CCNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
25034110 188874 None 0 Human Functional pIC50 = 5.5 5.5 1 3
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL505453 188874 None 0 Human Functional pIC50 = 5.5 5.5 1 3
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
11584660 93321 None 8 Human Functional pIC50 = 5.5 5.5 -19 5
Antagonist activity at human muscarinic receptor M3Antagonist activity at human muscarinic receptor M3
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
CHEMBL244946 93321 None 8 Human Functional pIC50 = 5.5 5.5 -19 5
Antagonist activity at human muscarinic receptor M3Antagonist activity at human muscarinic receptor M3
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
44573371 187593 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.7 Cc1ccc(-c2cccc(CN3CCNCC3)c2)cc1CNC(=O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494131 187593 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.7 Cc1ccc(-c2cccc(CN3CCNCC3)c2)cc1CNC(=O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
57758634 106519 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 421 6 0 1 6.5 C[N+]1(Cc2ccccc2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084465 106519 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 421 6 0 1 6.5 C[N+]1(Cc2ccccc2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140095 106519 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 421 6 0 1 6.5 C[N+]1(Cc2ccccc2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11431874 74307 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2023763 74307 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
145958111 162109 None 0 Human Functional pIC50 = 7.5 7.5 -3 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21)CN 10.1021/acsmedchemlett.7b00406
CHEMBL4159607 162109 None 0 Human Functional pIC50 = 7.5 7.5 -3 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21)CN 10.1021/acsmedchemlett.7b00406
71463136 83969 None 0 Human Functional pIC50 = 7.5 7.5 2 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 12 4 5 5.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(Cc3ccc(Cl)cc3)CCCCC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206608 83969 None 0 Human Functional pIC50 = 7.5 7.5 2 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 12 4 5 5.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(Cc3ccc(Cl)cc3)CCCCC2)cc1 10.1016/j.bmcl.2012.09.085
76320690 106516 None 0 Human Functional pIC50 = 6.5 6.5 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085063 106516 None 0 Human Functional pIC50 = 6.5 6.5 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140092 106516 None 0 Human Functional pIC50 = 6.5 6.5 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
6908726 109021 None 3 Rat Functional pIC50 = 6.5 6.5 - 1
Agonist activity at endothelial M3 receptor in Wistar-Kyoto rat thoracic aortic rings assessed as inhibition of phenylephrine-induced contractionAgonist activity at endothelial M3 receptor in Wistar-Kyoto rat thoracic aortic rings assessed as inhibition of phenylephrine-induced contraction
ChEMBL 274 3 1 5 2.2 O=C(N/N=C/c1ccsc1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2018.07.015
CHEMBL3211778 109021 None 3 Rat Functional pIC50 = 6.5 6.5 - 1
Agonist activity at endothelial M3 receptor in Wistar-Kyoto rat thoracic aortic rings assessed as inhibition of phenylephrine-induced contractionAgonist activity at endothelial M3 receptor in Wistar-Kyoto rat thoracic aortic rings assessed as inhibition of phenylephrine-induced contraction
ChEMBL 274 3 1 5 2.2 O=C(N/N=C/c1ccsc1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2018.07.015
42626096 12749 None 0 Human Functional pIC50 = 4.4 4.4 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1ccc(C(O)(c2ccc(OC)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1187802 12749 None 0 Human Functional pIC50 = 4.4 4.4 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1ccc(C(O)(c2ccc(OC)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL521921 12749 None 0 Human Functional pIC50 = 4.4 4.4 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1ccc(C(O)(c2ccc(OC)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
137647734 157938 None 0 Human Functional pIC50 = 6.4 6.4 -2 5
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 448 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4083681 157938 None 0 Human Functional pIC50 = 6.4 6.4 -2 5
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 448 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
44234683 106560 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1ccc(F)cc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cc(F)ccc1C 10.1021/jm900736e
CHEMBL3084406 106560 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1ccc(F)cc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cc(F)ccc1C 10.1021/jm900736e
CHEMBL3140205 106560 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1ccc(F)cc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cc(F)ccc1C 10.1021/jm900736e
46830361 7893 None 0 Human Functional pIC50 = 5.4 5.4 -10 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 433 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3c(F)c(F)c(F)c(F)c3F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090094 7893 None 0 Human Functional pIC50 = 5.4 5.4 -10 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 433 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3c(F)c(F)c(F)c(F)c3F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
137637944 155905 None 0 Human Functional pIC50 = 6.4 6.4 -3 5
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4059829 155905 None 0 Human Functional pIC50 = 6.4 6.4 -3 5
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
11364984 187367 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 444 6 2 6 3.2 C[C@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)n2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL492701 187367 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 444 6 2 6 3.2 C[C@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)n2)CCN1 10.1016/j.bmcl.2009.01.098
44590169 188350 None 0 Human Functional pIC50 = 7.4 7.4 -7 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 603 11 3 7 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL499565 188350 None 0 Human Functional pIC50 = 7.4 7.4 -7 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 603 11 3 7 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL539885 188350 None 0 Human Functional pIC50 = 7.4 7.4 -7 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 603 11 3 7 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
11606547 12604 None 0 Human Functional pIC50 = 4.4 4.4 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 484 8 1 2 6.4 CC(C)(C)c1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1186941 12604 None 0 Human Functional pIC50 = 4.4 4.4 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 484 8 1 2 6.4 CC(C)(C)c1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL483253 12604 None 0 Human Functional pIC50 = 4.4 4.4 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 484 8 1 2 6.4 CC(C)(C)c1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
71463134 83958 None 0 Human Functional pIC50 = 6.4 6.4 2 2
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 618 11 3 6 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N(C)Cc2n(C)cc[n+]2Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206594 83958 None 0 Human Functional pIC50 = 6.4 6.4 2 2
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 618 11 3 6 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N(C)Cc2n(C)cc[n+]2Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
44589574 172791 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 582 11 4 6 3.9 CCN(CC)C(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450093 172791 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 582 11 4 6 3.9 CCN(CC)C(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44573543 187595 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1C(F)(F)F 10.1016/j.bmcl.2009.01.098
CHEMBL494151 187595 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1C(F)(F)F 10.1016/j.bmcl.2009.01.098
11399125 193262 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 471 6 1 5 3.7 CC(=O)N1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL523012 193262 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 471 6 1 5 3.7 CC(=O)N1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
11619198 106547 None 0 Human Functional pIC50 = 8.3 8.3 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 365 4 0 2 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085058 106547 None 0 Human Functional pIC50 = 8.3 8.3 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 365 4 0 2 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140170 106547 None 0 Human Functional pIC50 = 8.3 8.3 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 365 4 0 2 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
137655063 159065 None 0 Human Functional pIC50 = 6.4 6.4 -3 5
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096143 159065 None 0 Human Functional pIC50 = 6.4 6.4 -3 5
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
76313454 106563 None 0 Human Functional pIC50 = 6.4 6.4 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085064 106563 None 0 Human Functional pIC50 = 6.4 6.4 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140214 106563 None 0 Human Functional pIC50 = 6.4 6.4 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
122195453 124177 None 0 Human Functional pIC50 = 5.4 5.4 -2 2
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633663 124177 None 0 Human Functional pIC50 = 5.4 5.4 -2 2
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
71450662 84040 None 0 Human Functional pIC50 = 6.4 6.4 -1 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 611 13 4 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2207176 84040 None 0 Human Functional pIC50 = 6.4 6.4 -1 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 611 13 4 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2012.09.085
122195446 124176 None 0 Human Functional pIC50 = 5.4 5.4 -1 5
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
CHEMBL3633656 124176 None 0 Human Functional pIC50 = 5.4 5.4 -1 5
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
76324334 106533 None 0 Human Functional pIC50 = 7.4 7.4 -2 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 369 4 0 3 4.5 Cc1ccoc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085070 106533 None 0 Human Functional pIC50 = 7.4 7.4 -2 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 369 4 0 3 4.5 Cc1ccoc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3140112 106533 None 0 Human Functional pIC50 = 7.4 7.4 -2 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 369 4 0 3 4.5 Cc1ccoc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
46830362 7896 None 0 Human Functional pIC50 = 5.4 5.4 -8 5
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)ccc3C(F)(F)F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090097 7896 None 0 Human Functional pIC50 = 5.4 5.4 -8 5
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)ccc3C(F)(F)F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
76327902 103554 None 0 Human Functional pIC50 = 6.4 6.4 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 354 4 0 4 4.4 Cc1ccoc1CN(C(=O)O[C@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085088 103554 None 0 Human Functional pIC50 = 6.4 6.4 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 354 4 0 4 4.4 Cc1ccoc1CN(C(=O)O[C@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
46883796 7895 None 0 Human Functional pIC50 = 5.4 5.4 -1 4
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 411 4 1 3 4.8 CCN1CCN(c2ccc(NC(=O)c3cccc(C(F)(F)F)c3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090096 7895 None 0 Human Functional pIC50 = 5.4 5.4 -1 4
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 411 4 1 3 4.8 CCN1CCN(c2ccc(NC(=O)c3cccc(C(F)(F)F)c3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
71463135 83968 None 0 Human Functional pIC50 = 7.4 7.4 2 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 607 12 4 5 5.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(Cc3ccc(Cl)cc3)CCCC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206607 83968 None 0 Human Functional pIC50 = 7.4 7.4 2 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 607 12 4 5 5.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(Cc3ccc(Cl)cc3)CCCC2)cc1 10.1016/j.bmcl.2012.09.085
71455968 83960 None 0 Human Functional pIC50 = 7.3 7.3 2 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206599 83960 None 0 Human Functional pIC50 = 7.3 7.3 2 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
11168935 187469 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 C[C@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493329 187469 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 C[C@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
44589496 186087 None 0 Human Functional pIC50 = 8.3 8.3 15 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 10 5 7 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL486983 186087 None 0 Human Functional pIC50 = 8.3 8.3 15 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 10 5 7 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5076445 216929 None 0 Rat Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CCN3C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5081816 217258 None 0 Rat Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
11215075 187443 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 C[C@@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493131 187443 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 C[C@@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
11410490 187705 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494741 187705 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.01.098
11249473 187788 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL495172 187788 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44590175 188739 None 0 Human Functional pIC50 = 7.3 7.3 -3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 3 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL503025 188739 None 0 Human Functional pIC50 = 7.3 7.3 -3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 3 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL553433 188739 None 0 Human Functional pIC50 = 7.3 7.3 -3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 3 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590035 191863 None 0 Human Functional pIC50 = 7.3 7.3 3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3OC)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL519760 191863 None 0 Human Functional pIC50 = 7.3 7.3 3 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3OC)C2)cc1 10.1016/j.bmcl.2008.09.020
152278786 182858 None 1 Human Functional pIC50 = 7.3 7.3 -30 4
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
CHEMBL4790083 182858 None 1 Human Functional pIC50 = 7.3 7.3 -30 4
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
71452455 83953 None 0 Human Functional pIC50 = 7.3 7.3 3 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 565 9 3 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(CC3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206588 83953 None 0 Human Functional pIC50 = 7.3 7.3 3 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 565 9 3 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(CC3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.09.085
44573305 187368 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 449 6 2 6 3.9 C[C@H]1CN(Cc2ccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)s2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL492702 187368 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 449 6 2 6 3.9 C[C@H]1CN(Cc2ccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)s2)CCN1 10.1016/j.bmcl.2009.01.098
11398832 187717 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 1 5 3.8 CN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL494781 187717 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 1 5 3.8 CN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44573620 187741 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 469 7 2 4 4.6 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494953 187741 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 469 7 2 4 4.6 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2009.01.098
44573499 187825 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1ccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)cc1 10.1016/j.bmcl.2009.01.098
CHEMBL495360 187825 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1ccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)cc1 10.1016/j.bmcl.2009.01.098
44573466 193421 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1ccccc1C(=O)NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL524168 193421 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1ccccc1C(=O)NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1 10.1016/j.bmcl.2009.01.098
44589569 172835 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 11 5 6 3.5 CCCNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450685 172835 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 11 5 6 3.5 CCCNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589572 189093 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 602 10 5 6 4.6 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)Nc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL508556 189093 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 602 10 5 6 4.6 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)Nc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
162657046 180949 None 0 Human Functional pIC50 = 6.3 6.3 -79 4
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@H](C)C1 10.1021/acsmedchemlett.0c00626
CHEMBL4757103 180949 None 0 Human Functional pIC50 = 6.3 6.3 -79 4
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@H](C)C1 10.1021/acsmedchemlett.0c00626
44573786 187415 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 5 2 5 3.1 O=C(NCc1cccc(-c2cccc(C(=O)N3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL492989 187415 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 5 2 5 3.1 O=C(NCc1cccc(-c2cccc(C(=O)N3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
71454215 83959 None 0 Human Functional pIC50 = 7.3 7.3 3 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 714 13 4 6 6.5 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCc2n(Cc3ccc(Cl)cc3)cc[n+]2Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206595 83959 None 0 Human Functional pIC50 = 7.3 7.3 3 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 714 13 4 6 6.5 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCc2n(Cc3ccc(Cl)cc3)cc[n+]2Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
122195454 124179 None 0 Human Functional pIC50 = 4.3 4.3 -8 2
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633665 124179 None 0 Human Functional pIC50 = 4.3 4.3 -8 2
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
122195453 124177 None 0 Human Functional pIC50 = 4.3 4.3 -2 2
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633663 124177 None 0 Human Functional pIC50 = 4.3 4.3 -2 2
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
10092649 193182 None 43 Rat Functional pIC50 = 5.3 5.3 -69 11
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 193182 None 43 Rat Functional pIC50 = 5.3 5.3 -69 11
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
10092649 193182 None 43 Rat Functional pIC50 = 5.3 5.3 -69 11
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 193182 None 43 Rat Functional pIC50 = 5.3 5.3 -69 11
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
152278786 182858 None 1 Human Functional pIC50 = 7.3 7.3 -30 4
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
CHEMBL4790083 182858 None 1 Human Functional pIC50 = 7.3 7.3 -30 4
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
76327900 106539 None 0 Human Functional pIC50 = 7.3 7.3 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085061 106539 None 0 Human Functional pIC50 = 7.3 7.3 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140142 106539 None 0 Human Functional pIC50 = 7.3 7.3 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
3156646 8266 None 6 Human Functional pIC50 = 5.3 5.3 -6 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 4 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3OC)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1092460 8266 None 6 Human Functional pIC50 = 5.3 5.3 -6 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 4 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3OC)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
76309757 103553 None 0 Human Functional pIC50 = 7.2 7.2 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 340 4 0 4 4.0 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085087 103553 None 0 Human Functional pIC50 = 7.2 7.2 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 340 4 0 4 4.0 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
122195446 124176 None 0 Human Functional pIC50 = 4.2 4.2 -1 5
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
CHEMBL3633656 124176 None 0 Human Functional pIC50 = 4.2 4.2 -1 5
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
71454217 83962 None 0 Human Functional pIC50 = 6.2 6.2 -1 2
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 551 9 3 5 4.3 CC[N+]1(C2CCN(C(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)CC2)CCCC1 10.1016/j.bmcl.2012.09.085
CHEMBL2206601 83962 None 0 Human Functional pIC50 = 6.2 6.2 -1 2
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 551 9 3 5 4.3 CC[N+]1(C2CCN(C(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)CC2)CCCC1 10.1016/j.bmcl.2012.09.085
122195454 124179 None 0 Human Functional pIC50 = 4.2 4.2 -8 2
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633665 124179 None 0 Human Functional pIC50 = 4.2 4.2 -8 2
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
71450616 83967 None 0 Human Functional pIC50 = 8.2 8.2 2 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 591 11 4 5 4.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)C23CC4CC(CC(C4)C2)C3)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206606 83967 None 0 Human Functional pIC50 = 8.2 8.2 2 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 591 11 4 5 4.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)C23CC4CC(CC(C4)C2)C3)cc1 10.1016/j.bmcl.2012.09.085
11284402 192824 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1ccc(F)c(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL521986 192824 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1ccc(F)c(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44589583 172584 None 0 Human Functional pIC50 = 8.2 8.2 6 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 561 10 5 6 3.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL448294 172584 None 0 Human Functional pIC50 = 8.2 8.2 6 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 561 10 5 6 3.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555471 172584 None 0 Human Functional pIC50 = 8.2 8.2 6 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 561 10 5 6 3.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590168 172832 None 0 Human Functional pIC50 = 8.2 8.2 6 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450652 172832 None 0 Human Functional pIC50 = 8.2 8.2 6 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540399 172832 None 0 Human Functional pIC50 = 8.2 8.2 6 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44589584 188887 None 0 Human Functional pIC50 = 8.2 8.2 6 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 563 10 4 5 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL505651 188887 None 0 Human Functional pIC50 = 8.2 8.2 6 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 563 10 4 5 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540144 188887 None 0 Human Functional pIC50 = 8.2 8.2 6 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 563 10 4 5 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590122 192669 None 0 Human Functional pIC50 = 8.2 8.2 15 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 555 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C#N)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL521244 192669 None 0 Human Functional pIC50 = 8.2 8.2 15 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 555 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C#N)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
11626847 106532 None 0 Human Functional pIC50 = 8.2 8.2 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085068 106532 None 0 Human Functional pIC50 = 8.2 8.2 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3140111 106532 None 0 Human Functional pIC50 = 8.2 8.2 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
137655938 159076 None 0 Human Functional pIC50 = 6.2 6.2 -64 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 362 6 2 4 3.0 NC/C=C\CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4096305 159076 None 0 Human Functional pIC50 = 6.2 6.2 -64 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 362 6 2 4 3.0 NC/C=C\CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL5081816 217258 None 0 Rat Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44573785 187413 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 6 1 5 4.2 CN1CCCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL492987 187413 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 6 1 5 4.2 CN1CCCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44573544 193348 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2009.01.098
CHEMBL523712 193348 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2009.01.098
44573421 187716 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 5 2 5 3.7 O=C(Nc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494779 187716 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 5 2 5 3.7 O=C(Nc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44573745 187756 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 6 1 4 5.0 O=C(NCc1cccc(-c2cccc(CN3CCCCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494997 187756 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 6 1 4 5.0 O=C(NCc1cccc(-c2cccc(CN3CCCCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
58975257 103432 None 0 Human Functional pIC50 = 5.2 5.2 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 377 6 2 2 3.9 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(N)=O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084638 103432 None 0 Human Functional pIC50 = 5.2 5.2 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 377 6 2 2 3.9 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(N)=O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
57758619 106548 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 499 15 0 1 9.2 CCCCCCCCCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084469 106548 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 499 15 0 1 9.2 CCCCCCCCCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140171 106548 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 499 15 0 1 9.2 CCCCCCCCCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44232706 106522 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1c(F)cccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cccc(F)c1C 10.1021/jm900736e
CHEMBL3084405 106522 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1c(F)cccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cccc(F)c1C 10.1021/jm900736e
CHEMBL3140098 106522 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1c(F)cccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cccc(F)c1C 10.1021/jm900736e
44234686 106535 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 4 1 3 5.1 Cc1cc(C(O)(C[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2csc(C)c2)cs1 10.1021/jm900736e
CHEMBL3084412 106535 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 4 1 3 5.1 Cc1cc(C(O)(C[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2csc(C)c2)cs1 10.1021/jm900736e
CHEMBL3140114 106535 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 4 1 3 5.1 Cc1cc(C(O)(C[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2csc(C)c2)cs1 10.1021/jm900736e
137654353 159108 None 0 Human Functional pIC50 = 6.2 6.2 -1 6
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096589 159108 None 0 Human Functional pIC50 = 6.2 6.2 -1 6
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
71457770 83961 None 0 Human Functional pIC50 = 7.2 7.2 1 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 647 10 3 5 6.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC([N+]3(Cc4ccc(Cl)cc4)CCCC3)CC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206600 83961 None 0 Human Functional pIC50 = 7.2 7.2 1 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 647 10 3 5 6.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC([N+]3(Cc4ccc(Cl)cc4)CCCC3)CC2)cc1 10.1016/j.bmcl.2012.09.085
44233189 103456 None 0 Human Functional pIC50 = 6.2 6.2 -2 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 349 5 1 2 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084678 103456 None 0 Human Functional pIC50 = 6.2 6.2 -2 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 349 5 1 2 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233189 103456 None 0 Human Functional pIC50 = 6.2 6.2 -2 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 349 5 1 2 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084678 103456 None 0 Human Functional pIC50 = 6.2 6.2 -2 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 349 5 1 2 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
11602980 103557 None 0 Human Functional pIC50 = 8.1 8.1 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 5 4.6 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085091 103557 None 0 Human Functional pIC50 = 8.1 8.1 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 5 4.6 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
44590178 172841 None 0 Human Functional pIC50 = 8.1 8.1 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2cccc(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450781 172841 None 0 Human Functional pIC50 = 8.1 8.1 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2cccc(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540400 172841 None 0 Human Functional pIC50 = 8.1 8.1 -1 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2cccc(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590123 183966 None 0 Human Functional pIC50 = 8.1 8.1 15 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 564 10 4 6 4.3 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(Cl)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL480877 183966 None 0 Human Functional pIC50 = 8.1 8.1 15 3
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 564 10 4 6 4.3 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(Cl)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
71457771 83963 None 0 Human Functional pIC50 = 7.2 7.2 5 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 691 14 4 5 7.0 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(Cc2ccc(Cl)cc2)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206602 83963 None 0 Human Functional pIC50 = 7.2 7.2 5 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 691 14 4 5 7.0 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(Cc2ccc(Cl)cc2)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
52176747 159123 None 0 Human Functional pIC50 = 5.2 5.2 -16 8
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4096727 159123 None 0 Human Functional pIC50 = 5.2 5.2 -16 8
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
2986945 95108 None 4 Rat Functional pIC50 = 4.2 4.2 -63 5
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 371 6 1 3 4.1 CCN1CCN(c2ccc(NC(=O)CCc3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL255169 95108 None 4 Rat Functional pIC50 = 4.2 4.2 -63 5
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 371 6 1 3 4.1 CCN1CCN(c2ccc(NC(=O)CCc3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
76320692 106564 None 0 Human Functional pIC50 = 6.2 6.2 -2 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 390 4 0 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085065 106564 None 0 Human Functional pIC50 = 6.2 6.2 -2 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 390 4 0 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140215 106564 None 0 Human Functional pIC50 = 6.2 6.2 -2 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 390 4 0 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
76309755 103544 None 0 Human Functional pIC50 = 6.1 6.1 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085079 103544 None 0 Human Functional pIC50 = 6.1 6.1 1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44234681 106549 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C2 10.1021/jm900736e
CHEMBL3084404 106549 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C2 10.1021/jm900736e
CHEMBL3140172 106549 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C2 10.1021/jm900736e
76316970 103541 None 0 Human Functional pIC50 = 7.1 7.1 2 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 350 4 0 3 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085076 103541 None 0 Human Functional pIC50 = 7.1 7.1 2 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 350 4 0 3 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
145960175 162222 None 0 Human Functional pIC50 = 6.1 6.1 -27 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN)=C(\F)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4161528 162222 None 0 Human Functional pIC50 = 6.1 6.1 -27 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN)=C(\F)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
76313457 103546 None 0 Human Functional pIC50 = 6.1 6.1 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 380 5 0 4 4.5 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085080 103546 None 0 Human Functional pIC50 = 6.1 6.1 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 380 5 0 4 4.5 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
137638270 156969 None 0 Human Functional pIC50 = 6.1 6.1 -6 5
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4071900 156969 None 0 Human Functional pIC50 = 6.1 6.1 -6 5
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
44573465 187380 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1ccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)cc1 10.1016/j.bmcl.2009.01.098
CHEMBL492802 187380 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1ccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)cc1 10.1016/j.bmcl.2009.01.098
11410317 187414 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 441 6 2 5 3.6 O=C(NCc1cccc(-c2cccc(CN3C[C@@H]4C[C@H]3CN4)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL492988 187414 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 441 6 2 5 3.6 O=C(NCc1cccc(-c2cccc(CN3C[C@@H]4C[C@H]3CN4)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
11443944 187790 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL495180 187790 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL5076535 216933 None 0 Rat Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCCN(C)C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44573545 187706 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 403 6 2 3 3.8 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(F)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494742 187706 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 403 6 2 3 3.8 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(F)c1 10.1016/j.bmcl.2009.01.098
44590166 189525 None 0 Human Functional pIC50 = 6.1 6.1 3 2
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 468 9 4 6 2.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(CC)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL513228 189525 None 0 Human Functional pIC50 = 6.1 6.1 3 2
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 468 9 4 6 2.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(CC)C2)cc1 10.1016/j.bmcl.2008.09.020
44573422 187744 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 444 6 3 5 3.8 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494962 187744 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 444 6 3 5 3.8 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
71459691 83966 None 0 Human Functional pIC50 = 7.1 7.1 -5 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 723 14 4 5 8.0 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(Cc2ccc3ccccc3c2)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206605 83966 None 0 Human Functional pIC50 = 7.1 7.1 -5 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 723 14 4 5 8.0 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(Cc2ccc3ccccc3c2)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2012.09.085
1090202 8493 None 6 Human Functional pIC50 = 6.1 6.1 1 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 377 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3ccccc3Cl)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1094003 8493 None 6 Human Functional pIC50 = 6.1 6.1 1 3
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 377 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3ccccc3Cl)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
44233928 86108 None 0 Human Functional pIC50 = 6.1 6.1 -1 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 438 7 1 2 5.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2308786 86108 None 0 Human Functional pIC50 = 6.1 6.1 -1 3
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 438 7 1 2 5.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233928 86108 None 0 Human Functional pIC50 = 6.1 6.1 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 438 7 1 2 5.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2308786 86108 None 0 Human Functional pIC50 = 6.1 6.1 -1 3
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 438 7 1 2 5.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
57758624 106520 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084467 106520 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140096 106520 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11691471 12571 None 0 Human Functional pIC50 = 4.1 4.1 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 398 6 1 1 5.2 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1186783 12571 None 0 Human Functional pIC50 = 4.1 4.1 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 398 6 1 1 5.2 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL478070 12571 None 0 Human Functional pIC50 = 4.1 4.1 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 398 6 1 1 5.2 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCc3ccccc3)(CC1)CC2 10.1021/jm801601v
145951963 163097 None 0 Human Functional pIC50 = 5.1 5.1 -199 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN)=C(/F)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4175500 163097 None 0 Human Functional pIC50 = 5.1 5.1 -199 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN)=C(/F)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
11398062 106518 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 427 6 0 1 6.9 C[N+]1(CC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084464 106518 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 427 6 0 1 6.9 C[N+]1(CC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140094 106518 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 427 6 0 1 6.9 C[N+]1(CC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11692150 12634 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187107 12634 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL490651 12634 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
145950432 163047 None 0 Human Functional pIC50 = 5.0 5.0 -120 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21)=C(\F)CN 10.1021/acsmedchemlett.7b00406
CHEMBL4174727 163047 None 0 Human Functional pIC50 = 5.0 5.0 -120 2
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21)=C(\F)CN 10.1021/acsmedchemlett.7b00406
76313456 106565 None 0 Human Functional pIC50 = 6.0 6.0 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
CHEMBL3085066 106565 None 0 Human Functional pIC50 = 6.0 6.0 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
CHEMBL3140216 106565 None 0 Human Functional pIC50 = 6.0 6.0 -1 3
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
66875589 103445 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084662 103445 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11504490 192711 None 0 Human Functional pKd = 11 11.0 - 0
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
CHEMBL521523 192711 None 0 Human Functional pKd = 11 11.0 - 0
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
11504490 192711 None 0 Human Functional pKd = 11 11.0 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL521523 192711 None 0 Human Functional pKd = 11 11.0 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
25034186 203895 None 0 Human Functional pKd = 10.9 10.9 - 0
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 722 11 4 8 7.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC4CCCCC4)s3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
CHEMBL540396 203895 None 0 Human Functional pKd = 10.9 10.9 - 0
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 722 11 4 8 7.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC4CCCCC4)s3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
CHEMBL604842 203895 None 0 Human Functional pKd = 10.9 10.9 - 0
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 722 11 4 8 7.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC4CCCCC4)s3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
25195533 78417 None 2 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2103803 78417 None 2 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2110584 78417 None 2 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
25195533 78417 None 2 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2103803 78417 None 2 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2110584 78417 None 2 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
44589580 173251 None 0 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 635 10 5 7 5.3 C[N+]1(Cc2ccc(O)cc2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC3CCCCC3)s2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL452142 173251 None 0 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 635 10 5 7 5.3 C[N+]1(Cc2ccc(O)cc2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC3CCCCC3)s2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL553448 173251 None 0 Human Functional pKd = 10.7 10.7 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 635 10 5 7 5.3 C[N+]1(Cc2ccc(O)cc2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC3CCCCC3)s2)C1 10.1016/j.bmcl.2008.09.020
11533795 12622 None 0 Human Functional pKd = 10.6 10.6 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(F)c3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187076 12622 None 0 Human Functional pKd = 10.6 10.6 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(F)c3)(CC1)CC2 10.1021/jm801601v
CHEMBL489212 12622 None 0 Human Functional pKd = 10.6 10.6 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(F)c3)(CC1)CC2 10.1021/jm801601v
25034184 188504 None 0 Human Functional pKd = 10.6 10.6 - 0
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 676 11 4 7 6.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
CHEMBL501803 188504 None 0 Human Functional pKd = 10.6 10.6 - 0
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 676 11 4 7 6.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
CHEMBL539887 188504 None 0 Human Functional pKd = 10.6 10.6 - 0
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 676 11 4 7 6.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
11442669 74481 None 0 Human Functional pKd = 10.6 10.6 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2023760 74481 None 0 Human Functional pKd = 10.6 10.6 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2027876 74481 None 0 Human Functional pKd = 10.6 10.6 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11519069 3939 None 2 Human Functional pKd = 10.5 10.5 - 3
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
11519070 3939 None 2 Human Functional pKd = 10.5 10.5 - 3
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
11519070.0 3939 None 2 Human Functional pKd = 10.5 10.5 - 3
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
4816 3939 None 2 Human Functional pKd = 10.5 10.5 - 3
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
7354 3939 None 2 Human Functional pKd = 10.5 10.5 - 3
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
CHEMBL1187833 3939 None 2 Human Functional pKd = 10.5 10.5 - 3
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
DB09076 3939 None 2 Human Functional pKd = 10.5 10.5 - 3
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
11528123 192742 None 0 Human Functional pKd = 10.5 10.5 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 529 8 2 5 4.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL521696 192742 None 0 Human Functional pKd = 10.5 10.5 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 529 8 2 5 4.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
42626090 12621 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1187075 12621 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL489211 12621 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
42626094 12629 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3F)(CC1)CC2 10.1021/jm801601v
CHEMBL1187092 12629 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3F)(CC1)CC2 10.1021/jm801601v
CHEMBL490237 12629 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3F)(CC1)CC2 10.1021/jm801601v
11585117 12765 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Br)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187851 12765 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Br)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL523957 12765 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Br)cc3)(CC1)CC2 10.1021/jm801601v
70689729 74505 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 479 10 0 2 6.9 C[N+]1(CCCOCc2ccccc2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2021997 74505 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 479 10 0 2 6.9 C[N+]1(CCCOCc2ccccc2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2028006 74505 None 0 Human Functional pKd = 10.4 10.4 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 479 10 0 2 6.9 C[N+]1(CCCOCc2ccccc2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11753447 187457 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 459 7 2 4 4.4 CC(=O)c1cccc(C(=O)NCc2ccc(F)c(-c3cccc(CN4CCN[C@@H](C)C4)c3)c2)c1 10.1021/jm800935u
CHEMBL493265 187457 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 459 7 2 4 4.4 CC(=O)c1cccc(C(=O)NCc2ccc(F)c(-c3cccc(CN4CCN[C@@H](C)C4)c3)c2)c1 10.1021/jm800935u
11365314 187458 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 473 8 2 4 4.8 CCC(=O)c1cccc(C(=O)NCc2ccc(F)c(-c3cccc(CN4CCN[C@@H](C)C4)c3)c2)c1 10.1021/jm800935u
CHEMBL493266 187458 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 473 8 2 4 4.8 CCC(=O)c1cccc(C(=O)NCc2ccc(F)c(-c3cccc(CN4CCN[C@@H](C)C4)c3)c2)c1 10.1021/jm800935u
57758618 106529 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 359 5 0 1 5.3 CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084457 106529 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 359 5 0 1 5.3 CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140108 106529 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 359 5 0 1 5.3 CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
57758626 106545 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 373 6 0 1 5.7 CCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084458 106545 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 373 6 0 1 5.7 CCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140168 106545 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 373 6 0 1 5.7 CCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
57758627 106546 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084459 106546 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140169 106546 None 0 Human Functional pKd = 10.3 10.3 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44232952 103438 None 0 Human Functional pKd = 10.2 10.2 - 0
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084650 103438 None 0 Human Functional pKd = 10.2 10.2 - 0
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
11592005 12751 None 0 Human Functional pKd = 10.2 10.2 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1ccc(F)cc1)(c1ccc(F)cc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187807 12751 None 0 Human Functional pKd = 10.2 10.2 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1ccc(F)cc1)(c1ccc(F)cc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL522081 12751 None 0 Human Functional pKd = 10.2 10.2 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1ccc(F)cc1)(c1ccc(F)cc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
11649606 12757 None 0 Human Functional pKd = 10.2 10.2 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 462 8 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Cl)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187835 12757 None 0 Human Functional pKd = 10.2 10.2 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 462 8 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Cl)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL523474 12757 None 0 Human Functional pKd = 10.2 10.2 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 462 8 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Cl)cc3)(CC1)CC2 10.1021/jm801601v
11651006 189056 None 0 Human Functional pKd = 10.2 10.2 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 573 11 3 6 3.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(CCCO)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL508097 189056 None 0 Human Functional pKd = 10.2 10.2 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 573 11 3 6 3.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(CCCO)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
11519318 12748 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(F)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187800 12748 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(F)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL521781 12748 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(F)cc3)(CC1)CC2 10.1021/jm801601v
11693689 171031 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 620 10 2 4 5.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(Cc6ccccc6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL445527 171031 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 620 10 2 4 5.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(Cc6ccccc6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL554706 171031 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 620 10 2 4 5.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(Cc6ccccc6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
44573747 187823 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 543 9 2 5 3.5 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(C=O)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL495350 187823 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 543 9 2 5 3.5 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(C=O)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
70685520 74491 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 443 11 0 1 7.6 CCCCCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2021998 74491 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 443 11 0 1 7.6 CCCCCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2027937 74491 None 0 Human Functional pKd = 10.1 10.1 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 443 11 0 1 7.6 CCCCCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44233188 103309 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 5 1 2 3.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084419 103309 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 5 1 2 3.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44234688 106536 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 346 3 0 0 5.8 Cc1ccccc1C(=C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3084414 106536 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 346 3 0 0 5.8 Cc1ccccc1C(=C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3140115 106536 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 346 3 0 0 5.8 Cc1ccccc1C(=C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
11223598 106581 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084413 106581 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140264 106581 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
42626019 12569 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL1186756 12569 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL476434 12569 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
25195533 78417 None 2 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2103803 78417 None 2 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2110584 78417 None 2 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11586041 172787 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 572 10 2 4 4.9 CCC[N+]1(C)CCN(Cc2cccc(C(=O)NCc3ccc(F)c(-c4cccc(CN5CCN[C@@H](C)C5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL450060 172787 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 572 10 2 4 4.9 CCC[N+]1(C)CCN(Cc2cccc(C(=O)NCc3ccc(F)c(-c4cccc(CN5CCN[C@@H](C)C5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL540251 172787 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 572 10 2 4 4.9 CCC[N+]1(C)CCN(Cc2cccc(C(=O)NCc3ccc(F)c(-c4cccc(CN5CCN[C@@H](C)C5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44589581 188896 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 615 12 5 6 4.9 C=CC[N+]1(Cc2cccc(O)c2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC(C)C)cc2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL505751 188896 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 615 12 5 6 4.9 C=CC[N+]1(Cc2cccc(O)c2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC(C)C)cc2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL540145 188896 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 615 12 5 6 4.9 C=CC[N+]1(Cc2cccc(O)c2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC(C)C)cc2)C1 10.1016/j.bmcl.2008.09.020
44589579 189162 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 595 10 5 7 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)s1 10.1016/j.bmcl.2008.09.020
CHEMBL509515 189162 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 595 10 5 7 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)s1 10.1016/j.bmcl.2008.09.020
CHEMBL540148 189162 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 595 10 5 7 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)s1 10.1016/j.bmcl.2008.09.020
44233930 106580 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 363 5 1 1 3.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084409 106580 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 363 5 1 1 3.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140263 106580 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 363 5 1 1 3.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
42626017 12767 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(Br)c3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187854 12767 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(Br)c3)(CC1)CC2 10.1021/jm801601v
CHEMBL524119 12767 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(Br)c3)(CC1)CC2 10.1021/jm801601v
25034182 172687 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL448870 172687 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL540359 172687 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
11585987 187824 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 516 8 2 5 4.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCOCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL495358 187824 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 516 8 2 5 4.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCOCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
11607628 188419 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 584 8 2 4 5.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+]6(CCCCC6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL500560 188419 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 584 8 2 4 5.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+]6(CCCCC6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL539886 188419 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 584 8 2 4 5.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+]6(CCCCC6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
25034182 172687 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL448870 172687 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540359 172687 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
25132856 187322 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 515 8 3 5 3.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
CHEMBL492437 187322 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 515 8 3 5 3.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
25132856 187322 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 515 8 3 5 3.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL492437 187322 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 515 8 3 5 3.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
11556983 187471 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 544 8 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493331 187471 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 544 8 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL538864 187471 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 544 8 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL555476 187471 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 544 8 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
57758616 106530 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 398 7 0 2 5.6 C[N+]1(CCCC#N)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084463 106530 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 398 7 0 2 5.6 C[N+]1(CCCC#N)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140109 106530 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 398 7 0 2 5.6 C[N+]1(CCCC#N)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
57758629 106552 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 375 6 1 2 4.3 C[N+]1(CCO)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084460 106552 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 375 6 1 2 4.3 C[N+]1(CCO)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140180 106552 None 0 Human Functional pKd = 9.8 9.8 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 375 6 1 2 4.3 C[N+]1(CCO)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11535362 187724 None 0 Human Functional pKd = 9.7 9.7 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 545 12 2 5 4.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN(C)CCCN(C)C)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL494837 187724 None 0 Human Functional pKd = 9.7 9.7 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 545 12 2 5 4.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN(C)CCCN(C)C)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
16086059 80806 None 0 Rat Functional pKd = 9.7 9.7 - 0
Antagonist activity at M3 receptor assessed as inhibition of carbachol-induced contraction of rat tracheaAntagonist activity at M3 receptor assessed as inhibition of carbachol-induced contraction of rat trachea
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL215180 80806 None 0 Rat Functional pKd = 9.7 9.7 - 0
Antagonist activity at M3 receptor assessed as inhibition of carbachol-induced contraction of rat tracheaAntagonist activity at M3 receptor assessed as inhibition of carbachol-induced contraction of rat trachea
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
11249888 187483 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 442 6 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C#N)c4)ccc3F)c2)CCN1 10.1021/jm800935u
CHEMBL493465 187483 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 442 6 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C#N)c4)ccc3F)c2)CCN1 10.1021/jm800935u
11642407 12624 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1cccc(F)c1)(c1cccc(F)c1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187079 12624 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1cccc(F)c1)(c1cccc(F)c1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL489625 12624 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1cccc(F)c1)(c1cccc(F)c1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
11564285 193264 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 543 8 2 5 4.4 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCCN(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL523044 193264 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 543 8 2 5 4.4 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCCN(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
44232952 103438 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084650 103438 None 0 Human Functional pKd = 9.5 9.5 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11519069 3939 None 2 Human Functional pKd = 9.5 9.5 - 3
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
11519070 3939 None 2 Human Functional pKd = 9.5 9.5 - 3
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
11519070.0 3939 None 2 Human Functional pKd = 9.5 9.5 - 3
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
4816 3939 None 2 Human Functional pKd = 9.5 9.5 - 3
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
7354 3939 None 2 Human Functional pKd = 9.5 9.5 - 3
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
CHEMBL1187833 3939 None 2 Human Functional pKd = 9.5 9.5 - 3
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
DB09076 3939 None 2 Human Functional pKd = 9.5 9.5 - 3
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
42625938 12620 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 337 5 2 2 2.9 NCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187073 12620 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 337 5 2 2 2.9 NCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL489032 12620 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 337 5 2 2 2.9 NCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
15951517 12631 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 8 1 2 4.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
CHEMBL1187094 12631 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 8 1 2 4.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
CHEMBL490243 12631 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 8 1 2 4.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
11512119 12758 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 453 8 1 3 5.0 N#Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1187838 12758 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 453 8 1 3 5.0 N#Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL523598 12758 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 453 8 1 3 5.0 N#Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
69058946 106531 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084658 106531 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140110 106531 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
69058946 106531 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084658 106531 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3140110 106531 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
42625944 12609 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 426 8 1 1 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1186964 12609 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 426 8 1 1 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL484475 12609 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 426 8 1 1 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCc3ccccc3)(CC1)CC2 10.1021/jm801601v
16041939 12632 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 423 8 0 2 5.3 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
CHEMBL1187095 12632 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 423 8 0 2 5.3 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
CHEMBL490244 12632 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 423 8 0 2 5.3 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
57758617 106517 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 389 7 0 2 4.9 COCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084462 106517 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 389 7 0 2 4.9 COCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140093 106517 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 389 7 0 2 4.9 COCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11636578 193186 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 514 8 2 4 5.2 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCCCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL522495 193186 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 514 8 2 4 5.2 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCCCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
44589582 171744 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 12 4 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](CC3CC3)(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL446587 171744 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 12 4 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](CC3CC3)(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL550885 171744 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 12 4 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](CC3CC3)(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589576 189164 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 6 5 3.9 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL509520 189164 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 6 5 3.9 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555706 189164 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 6 5 3.9 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
57758613 106556 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 433 10 0 3 4.9 COCCOCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084468 106556 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 433 10 0 3 4.9 COCCOCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140184 106556 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 433 10 0 3 4.9 COCCOCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11705920 12753 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 7 1 2 5.0 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187810 12753 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 7 1 2 5.0 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL522418 12753 None 0 Human Functional pKd = 9.1 9.1 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 7 1 2 5.0 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
11633226 106584 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 344 3 0 2 5.6 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084418 106584 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 344 3 0 2 5.6 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140267 106584 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 344 3 0 2 5.6 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
11223598 106581 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084413 106581 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140264 106581 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
11691950 12766 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187853 12766 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL524097 12766 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
57758623 106554 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 371 6 0 1 5.5 C=CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084461 106554 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 371 6 0 1 5.5 C=CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140182 106554 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 371 6 0 1 5.5 C=CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44234690 106583 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 4 1 1 4.7 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084417 106583 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 4 1 1 4.7 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140266 106583 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 4 1 1 4.7 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44232949 106582 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 362 4 1 3 4.8 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084415 106582 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 362 4 1 3 4.8 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140265 106582 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 362 4 1 3 4.8 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
11635210 12740 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 458 9 1 3 5.1 COc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL1187765 12740 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 458 9 1 3 5.1 COc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL519652 12740 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 458 9 1 3 5.1 COc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
44589578 173273 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1nc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)no1 10.1016/j.bmcl.2008.09.020
CHEMBL452193 173273 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1nc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)no1 10.1016/j.bmcl.2008.09.020
CHEMBL540401 173273 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1nc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)no1 10.1016/j.bmcl.2008.09.020
44589577 189076 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1noc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)n1 10.1016/j.bmcl.2008.09.020
CHEMBL508343 189076 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1noc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)n1 10.1016/j.bmcl.2008.09.020
CHEMBL540146 189076 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1noc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)n1 10.1016/j.bmcl.2008.09.020
44232702 106559 None 0 Human Functional pKd = 8 8.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3084401 106559 None 0 Human Functional pKd = 8 8.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3140203 106559 None 0 Human Functional pKd = 8 8.0 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
11692150 12634 None 0 Human Functional pKd = 8 8.0 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187107 12634 None 0 Human Functional pKd = 8 8.0 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL490651 12634 None 0 Human Functional pKd = 8 8.0 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
25034182 172687 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL448870 172687 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL540359 172687 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
76327869 103306 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 333 4 1 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084396 103306 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 333 4 1 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
66875589 103445 None 0 Human Functional pKd = 8.6 8.6 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084662 103445 None 0 Human Functional pKd = 8.6 8.6 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11235700 106523 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084410 106523 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140099 106523 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
66875589 103445 None 0 Human Functional pKd = 8.6 8.6 - 1
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084662 103445 None 0 Human Functional pKd = 8.6 8.6 - 1
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
44233192 106538 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084643 106538 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3140141 106538 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
42626088 12628 None 0 Human Functional pKd = 8.5 8.5 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
CHEMBL1187091 12628 None 0 Human Functional pKd = 8.5 8.5 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
CHEMBL490236 12628 None 0 Human Functional pKd = 8.5 8.5 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
42626013 12630 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 437 8 0 2 5.7 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187093 12630 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 437 8 0 2 5.7 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL490242 12630 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 437 8 0 2 5.7 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
11722039 187470 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 530 8 3 4 3.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C[N+]5(C)CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493330 187470 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 530 8 3 4 3.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C[N+]5(C)CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL558605 187470 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 530 8 3 4 3.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C[N+]5(C)CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
11650778 187578 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 474 8 2 4 4.3 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN(C)C)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL494022 187578 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 474 8 2 4 4.3 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN(C)C)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
16042745 185407 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 551 8 4 5 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+]3(CCCCCC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL485932 185407 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 551 8 4 5 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+]3(CCCCCC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL538360 185407 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 551 8 4 5 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+]3(CCCCCC3)C2)cc1 10.1016/j.bmcl.2008.09.020
44233190 103457 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084679 103457 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233192 106538 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084643 106538 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140141 106538 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233190 103457 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084679 103457 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
42626092 12639 None 0 Human Functional pKd = 8.4 8.4 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187132 12639 None 0 Human Functional pKd = 8.4 8.4 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL491246 12639 None 0 Human Functional pKd = 8.4 8.4 - 1
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
66604762 106566 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 318 3 0 0 5.1 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084398 106566 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 318 3 0 0 5.1 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140217 106566 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 318 3 0 0 5.1 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44232700 106567 None 0 Human Functional pKd = 8.3 8.3 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3084399 106567 None 0 Human Functional pKd = 8.3 8.3 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3140218 106567 None 0 Human Functional pKd = 8.3 8.3 - 1
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
16065402 67949 None 0 Human Functional pKi = 10.3 10.3 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 428 9 1 3 4.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910848 67949 None 0 Human Functional pKi = 10.3 10.3 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 428 9 1 3 4.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2)C1 10.1021/jm200884j
367 3824 None 10 Human Functional pKi = 10.3 10.3 -3 8
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
5487427 3824 None 10 Human Functional pKi = 10.3 10.3 -3 8
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
5487427.0 3824 None 10 Human Functional pKi = 10.3 10.3 -3 8
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
8592 3824 None 10 Human Functional pKi = 10.3 10.3 -3 8
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL1900528 3824 None 10 Human Functional pKi = 10.3 10.3 -3 8
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL3305968 3824 None 10 Human Functional pKi = 10.3 10.3 -3 8
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL4650755 3824 None 10 Human Functional pKi = 10.3 10.3 -3 8
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
DB01409 3824 None 10 Human Functional pKi = 10.3 10.3 -3 8
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
54757541 67953 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2O)C1 10.1021/jm200884j
CHEMBL1910852 67953 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2O)C1 10.1021/jm200884j
54757856 67958 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 10 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(OCc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910857 67958 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 10 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(OCc2cccc(O)c2)C1 10.1021/jm200884j
325 2062 None 10 Human Functional pKi = 9.7 9.7 1 3
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1021/jm200884j
3746 2062 None 10 Human Functional pKi = 9.7 9.7 1 3
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1021/jm200884j
657308 2062 None 10 Human Functional pKi = 9.7 9.7 1 3
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1021/jm200884j
CHEMBL1615433 2062 None 10 Human Functional pKi = 9.7 9.7 1 3
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1021/jm200884j
DB00332 2062 None 10 Human Functional pKi = 9.7 9.7 1 3
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1021/jm200884j
16065403 67957 None 24 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910856 67957 None 24 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1 10.1021/jm200884j
16034837 67952 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910851 67952 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
16065543 67963 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 478 9 2 4 5.1 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)cc(Cl)c2)C1 10.1021/jm200884j
CHEMBL1910862 67963 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 478 9 2 4 5.1 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)cc(Cl)c2)C1 10.1021/jm200884j
16065135 67947 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910846 67947 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2)C1 10.1021/jm200884j
16065407 67966 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2F)C1 10.1021/jm200884j
CHEMBL1910865 67966 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2F)C1 10.1021/jm200884j
16065268 67950 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 456 9 1 3 5.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2ccccc2)CC1 10.1021/jm200884j
CHEMBL1910849 67950 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 456 9 1 3 5.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2ccccc2)CC1 10.1021/jm200884j
16065137 67951 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910850 67951 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
54757544 67961 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 476 9 2 4 5.0 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cc(O)cc(F)c2)C1 10.1021/jm200884j
CHEMBL1910860 67961 None 0 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 476 9 2 4 5.0 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cc(O)cc(F)c2)C1 10.1021/jm200884j
16065405 67964 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)cc(F)c2)C1 10.1021/jm200884j
CHEMBL1910863 67964 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)cc(F)c2)C1 10.1021/jm200884j
16065541 67967 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)ccc2F)C1 10.1021/jm200884j
CHEMBL1910866 67967 None 0 Human Functional pKi = 9.2 9.2 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)ccc2F)C1 10.1021/jm200884j
16065406 67959 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 470 9 2 4 5.0 NC(=O)C(CCC1(N2CC(Oc3cccc(O)c3)C2)CCCC1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
CHEMBL1910858 67959 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 470 9 2 4 5.0 NC(=O)C(CCC1(N2CC(Oc3cccc(O)c3)C2)CCCC1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
54757543 67954 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccc(O)cc2)C1 10.1021/jm200884j
CHEMBL1910853 67954 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccc(O)cc2)C1 10.1021/jm200884j
16065136 67948 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910847 67948 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2ccccc2)C1 10.1021/jm200884j
16065404 67962 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 478 9 2 4 5.1 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccc(Cl)c(O)c2)C1 10.1021/jm200884j
CHEMBL1910861 67962 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 478 9 2 4 5.1 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccc(Cl)c(O)c2)C1 10.1021/jm200884j
126534204 138519 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 504 7 1 7 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1cc[nH]c(=O)c1 10.1016/j.bmc.2016.02.031
CHEMBL3774411 138519 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 504 7 1 7 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1cc[nH]c(=O)c1 10.1016/j.bmc.2016.02.031
54757653 67956 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2O)C1 10.1021/jm200884j
CHEMBL1910855 67956 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2O)C1 10.1021/jm200884j
121304590 145446 None 0 Human Functional pKi = 5.9 5.9 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3913607 145446 None 0 Human Functional pKi = 5.9 5.9 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
121304477 152260 None 0 Human Functional pKi = 5.9 5.9 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 487 7 0 6 5.6 Cc1ncccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3968272 152260 None 0 Human Functional pKi = 5.9 5.9 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 487 7 0 6 5.6 Cc1ncccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
126534771 138680 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 424 7 0 8 3.5 Cc1ncoc1-c1nnc(SCCCN2CC3CCN(c4ccccc4)C3C2)n1C 10.1016/j.bmc.2016.02.031
CHEMBL3775589 138680 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 424 7 0 8 3.5 Cc1ncoc1-c1nnc(SCCCN2CC3CCN(c4ccccc4)C3C2)n1C 10.1016/j.bmc.2016.02.031
126533969 138555 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 427 7 0 7 3.4 Cn1c(SCCCN2CC3CCN(c4ccccc4)C3C2)nnc1C1CCOCC1 10.1016/j.bmc.2016.02.031
CHEMBL3774649 138555 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 427 7 0 7 3.4 Cn1c(SCCCN2CC3CCN(c4ccccc4)C3C2)nnc1C1CCOCC1 10.1016/j.bmc.2016.02.031
121304609 153050 None 0 Human Functional pKi = 5.8 5.8 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(F)cc3C(F)(F)F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3975147 153050 None 0 Human Functional pKi = 5.8 5.8 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(F)cc3C(F)(F)F)C2)n1C 10.1021/acs.jmedchem.6b00972
121304654 148965 None 0 Human Functional pKi = 6.7 6.7 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 530 8 1 7 4.7 Cc1nc(C(N)=O)ccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3941520 148965 None 0 Human Functional pKi = 6.7 6.7 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 530 8 1 7 4.7 Cc1nc(C(N)=O)ccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
121304538 150093 None 0 Human Functional pKi = 6.7 6.7 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 516 8 1 7 4.4 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)nc1 10.1021/acs.jmedchem.6b00972
CHEMBL3950254 150093 None 0 Human Functional pKi = 6.7 6.7 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 516 8 1 7 4.4 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)nc1 10.1021/acs.jmedchem.6b00972
54757542 67960 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 492 9 2 4 5.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccc(Cl)c(O)c2)C1 10.1021/jm200884j
CHEMBL1910859 67960 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 492 9 2 4 5.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccc(Cl)c(O)c2)C1 10.1021/jm200884j
16065269 67955 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 472 9 2 4 5.3 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2cccc(O)c2)CC1 10.1021/jm200884j
CHEMBL1910854 67955 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 472 9 2 4 5.3 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2cccc(O)c2)CC1 10.1021/jm200884j
54757332 67946 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 414 9 1 3 4.4 NC(=O)C(CCCN1CC[C@H](Oc2ccccc2)C1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
CHEMBL1910845 67946 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 414 9 1 3 4.4 NC(=O)C(CCCN1CC[C@H](Oc2ccccc2)C1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
121304458 154078 None 0 Human Functional pKi = 5.7 5.7 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 409 7 0 7 4.1 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccccc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3983937 154078 None 0 Human Functional pKi = 5.7 5.7 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 409 7 0 7 4.1 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccccc3)C2)n1C 10.1021/acs.jmedchem.6b00972
121304867 154288 None 0 Human Functional pKi = 5.7 5.7 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@H]3c3ccc(F)cc3C(F)(F)F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3985877 154288 None 0 Human Functional pKi = 5.7 5.7 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@H]3c3ccc(F)cc3C(F)(F)F)C2)n1C 10.1021/acs.jmedchem.6b00972
126534291 138628 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 488 7 0 7 4.6 Cn1c(SCCCN2CC3CCN(c4ccccc4C(F)(F)F)C3C2)nnc1-c1cccnc1 10.1016/j.bmc.2016.02.031
CHEMBL3775197 138628 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 488 7 0 7 4.6 Cn1c(SCCCN2CC3CCN(c4ccccc4C(F)(F)F)C3C2)nnc1-c1cccnc1 10.1016/j.bmc.2016.02.031
121304598 145334 None 0 Human Functional pKi = 6.6 6.6 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 535 8 1 6 5.4 CC(=O)NC1CCC(c2nnc(SCCCN3CC[C@]4(C[C@@H]4c4ccc(C(F)(F)F)cc4)C3)n2C)CC1 10.1021/acs.jmedchem.6b00972
CHEMBL3912801 145334 None 0 Human Functional pKi = 6.6 6.6 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 535 8 1 6 5.4 CC(=O)NC1CCC(c2nnc(SCCCN3CC[C@]4(C[C@@H]4c4ccc(C(F)(F)F)cc4)C3)n2C)CC1 10.1021/acs.jmedchem.6b00972
126534373 138633 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 510 7 0 8 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4F)C3C2)n1C 10.1016/j.bmc.2016.02.031
CHEMBL3775226 138633 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 510 7 0 8 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4F)C3C2)n1C 10.1016/j.bmc.2016.02.031
121304464 144432 None 0 Human Functional pKi = 6.6 6.6 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 480 7 0 8 4.7 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1csnn1 10.1021/acs.jmedchem.6b00972
CHEMBL3905582 144432 None 0 Human Functional pKi = 6.6 6.6 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 480 7 0 8 4.7 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1csnn1 10.1021/acs.jmedchem.6b00972
121304485 148263 None 0 Human Functional pKi = 6.6 6.6 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3935692 148263 None 0 Human Functional pKi = 6.6 6.6 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
10125445 76055 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at muscarinic M3 receptorAntagonist activity at muscarinic M3 receptor
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1021/jm800582j
CHEMBL205654 76055 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at muscarinic M3 receptorAntagonist activity at muscarinic M3 receptor
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1021/jm800582j
121304452 149006 None 0 Human Functional pKi = 6.5 6.5 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 539 8 0 7 6.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(-c2ncco2)cc1 10.1021/acs.jmedchem.6b00972
CHEMBL3941818 149006 None 0 Human Functional pKi = 6.5 6.5 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 539 8 0 7 6.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(-c2ncco2)cc1 10.1021/acs.jmedchem.6b00972
121304574 143120 None 0 Human Functional pKi = 6.5 6.5 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 503 7 0 7 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccn(C)c(=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL3894853 143120 None 0 Human Functional pKi = 6.5 6.5 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 503 7 0 7 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccn(C)c(=O)c1 10.1021/acs.jmedchem.6b00972
121304441 152473 None 0 Human Functional pKi = 6.4 6.4 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL3970323 152473 None 0 Human Functional pKi = 6.4 6.4 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
121304408 143641 None 0 Human Functional pKi = 6.4 6.4 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)cc1 10.1021/acs.jmedchem.6b00972
CHEMBL3899125 143641 None 0 Human Functional pKi = 6.4 6.4 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)cc1 10.1021/acs.jmedchem.6b00972
121304649 150733 None 0 Human Functional pKi = 6.4 6.4 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3955505 150733 None 0 Human Functional pKi = 6.4 6.4 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
126535075 138566 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 518 7 0 8 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1ccc(=O)n(C)c1 10.1016/j.bmc.2016.02.031
CHEMBL3774769 138566 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 518 7 0 8 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1ccc(=O)n(C)c1 10.1016/j.bmc.2016.02.031
121304424 143931 None 0 Human Functional pKi = 6.3 6.3 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3901587 143931 None 0 Human Functional pKi = 6.3 6.3 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
134150754 151818 None 0 Human Functional pKi = 6.2 6.2 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 489 7 0 6 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1=CCC(=O)N=C1 10.1021/acs.jmedchem.6b00972
CHEMBL3964512 151818 None 0 Human Functional pKi = 6.2 6.2 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 489 7 0 6 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1=CCC(=O)N=C1 10.1021/acs.jmedchem.6b00972
134134147 143461 None 0 Human Functional pKi = 6.2 6.2 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 489 7 0 6 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1=CC=NC(=O)C1 10.1021/acs.jmedchem.6b00972
CHEMBL3897772 143461 None 0 Human Functional pKi = 6.2 6.2 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 489 7 0 6 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1=CC=NC(=O)C1 10.1021/acs.jmedchem.6b00972
134150637 151654 None 0 Human Functional pKi = 6.2 6.2 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 522 7 1 6 4.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCN(C(N)=O)CC1 10.1021/acs.jmedchem.6b00972
CHEMBL3963243 151654 None 0 Human Functional pKi = 6.2 6.2 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 522 7 1 6 4.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCN(C(N)=O)CC1 10.1021/acs.jmedchem.6b00972
54757766 67965 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 512 9 2 4 5.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)c(Cl)cc2Cl)C1 10.1021/jm200884j
CHEMBL1910864 67965 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 512 9 2 4 5.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)c(Cl)cc2Cl)C1 10.1021/jm200884j
483747 105465 None 1 Human Functional pKi = 6.1 6.1 - 1
Antagonistic activity against muscarinic M3 receptorAntagonistic activity against muscarinic M3 receptor
ChEMBL 503 4 0 5 4.9 Cc1ncnc(C)c1C(=O)N1CCC(C)(N2CCN([C@@H](C)c3ccc(C(F)(F)F)cc3)[C@@H](C)C2)CC1 10.1021/jm0304515
CHEMBL311795 105465 None 1 Human Functional pKi = 6.1 6.1 - 1
Antagonistic activity against muscarinic M3 receptorAntagonistic activity against muscarinic M3 receptor
ChEMBL 503 4 0 5 4.9 Cc1ncnc(C)c1C(=O)N1CCC(C)(N2CCN([C@@H](C)c3ccc(C(F)(F)F)cc3)[C@@H](C)C2)CC1 10.1021/jm0304515
121304500 149842 None 0 Human Functional pKi = 6.1 6.1 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 480 7 0 6 5.1 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCOCC1 10.1021/acs.jmedchem.6b00972
CHEMBL3948167 149842 None 0 Human Functional pKi = 6.1 6.1 - 0
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 480 7 0 6 5.1 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCOCC1 10.1021/acs.jmedchem.6b00972
3009352 96692 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonistic activity against muscarinic M3 receptorAntagonistic activity against muscarinic M3 receptor
ChEMBL 517 5 0 5 5.3 CC[C@@H](c1ccc(C(F)(F)F)cc1)N1CCN(C2(C)CCN(C(=O)c3c(C)ncnc3C)CC2)C[C@@H]1C 10.1021/jm0304515
CHEMBL263555 96692 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonistic activity against muscarinic M3 receptorAntagonistic activity against muscarinic M3 receptor
ChEMBL 517 5 0 5 5.3 CC[C@@H](c1ccc(C(F)(F)F)cc1)N1CCN(C2(C)CCN(C(=O)c3c(C)ncnc3C)CC2)C[C@@H]1C 10.1021/jm0304515
23724781 2835 None 13 Rat Functional pEC50 = 8.0 8.0 2 8
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
23724781.0 2835 None 13 Rat Functional pEC50 = 8.0 8.0 2 8
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
316 2835 None 13 Rat Functional pEC50 = 8.0 8.0 2 8
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
317 2835 None 13 Rat Functional pEC50 = 8.0 8.0 2 8
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
71183 2835 None 13 Rat Functional pEC50 = 8.0 8.0 2 8
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL1354199 2835 None 13 Rat Functional pEC50 = 8.0 8.0 2 8
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL3140030 2835 None 13 Rat Functional pEC50 = 8.0 8.0 2 8
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL376897 2835 None 13 Rat Functional pEC50 = 8.0 8.0 2 8
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
DB00462 2835 None 13 Rat Functional pEC50 = 8.0 8.0 2 8
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
1979 77355 None 47 Human Functional pEC50 = 8.3 8.3 -1 7
NoneNone
Drug Central 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
CHEMBL20835 77355 None 47 Human Functional pEC50 = 8.3 8.3 -1 7
NoneNone
Drug Central 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
187 255 None 24 Human Functional pEC50 = 8.2 8.2 -1 8
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
187.0 255 None 24 Human Functional pEC50 = 8.2 8.2 -1 8
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
294 255 None 24 Human Functional pEC50 = 8.2 8.2 -1 8
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
65 255 None 24 Human Functional pEC50 = 8.2 8.2 -1 8
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
8593 255 None 24 Human Functional pEC50 = 8.2 8.2 -1 8
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
CHEMBL667 255 None 24 Human Functional pEC50 = 8.2 8.2 -1 8
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
DB03128 255 None 24 Human Functional pEC50 = 8.2 8.2 -1 8
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
1726 2497 None 8 Rat Functional pEC50 = 8.2 8.2 -5 8
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
1993 2497 None 8 Rat Functional pEC50 = 8.2 8.2 -5 8
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
1993.0 2497 None 8 Rat Functional pEC50 = 8.2 8.2 -5 8
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
7438 2497 None 8 Rat Functional pEC50 = 8.2 8.2 -5 8
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
CHEMBL978 2497 None 8 Rat Functional pEC50 = 8.2 8.2 -5 8
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
DB06709 2497 None 8 Rat Functional pEC50 = 8.2 8.2 -5 8
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
2166 3123 None 33 Human Functional pEC50 = 8.2 8.2 -1 10
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
305 3123 None 33 Human Functional pEC50 = 8.2 8.2 -1 10
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
5910 3123 None 33 Human Functional pEC50 = 8.2 8.2 -1 10
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
5910.0 3123 None 33 Human Functional pEC50 = 8.2 8.2 -1 10
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
CHEMBL550 3123 None 33 Human Functional pEC50 = 8.2 8.2 -1 10
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
DB01085 3123 None 33 Human Functional pEC50 = 8.2 8.2 -1 10
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
123603 883 None 21 Human Functional pEC50 = 8.1 8.1 -1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
2684 883 None 21 Human Functional pEC50 = 8.1 8.1 -1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
2684.0 883 None 21 Human Functional pEC50 = 8.1 8.1 -1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
584 883 None 21 Human Functional pEC50 = 8.1 8.1 -1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
9658 883 None 21 Human Functional pEC50 = 8.1 8.1 -1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
CHEMBL168815 883 None 21 Human Functional pEC50 = 8.1 8.1 -1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
DB00185 883 None 21 Human Functional pEC50 = 8.1 8.1 -1 5
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
5831 218453 None 0 Human Functional pEC50 = 8.1 8.1 -1 5
NoneNone
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
5831.0 218453 None 0 Human Functional pEC50 = 8.1 8.1 -1 5
NoneNone
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
CHEMBL965 218453 None 0 Human Functional pEC50 = 8.1 8.1 -1 5
NoneNone
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
DB00411 218453 None 0 Human Functional pEC50 = 8.1 8.1 -1 5
NoneNone
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
3008304 4023 None 46 Human Functional pEC50 = 5.2 5.2 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 19438238
7632 4023 None 46 Human Functional pEC50 = 5.2 5.2 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 19438238
CHEMBL523685 4023 None 46 Human Functional pEC50 = 5.2 5.2 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 19438238
1726 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
1726 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
1993 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
1993 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
1993.0 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
1993.0 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
7438 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
7438 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
CHEMBL978 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
CHEMBL978 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
DB06709 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
DB06709 2497 None 8 Rat Functional pEC50 = 6.9 6.9 -5 8
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
288 252 None 0 Human Functional pEC50 None 5.1 5.1 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@H]1C[NH+]2CCC1CC2 8968358
6979053 252 None 0 Human Functional pEC50 None 5.1 5.1 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@H]1C[NH+]2CCC1CC2 8968358
286 251 None 0 Human Functional pEC50 None 5.7 5.7 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@@H]1C[NH+]2CCC1CC2 8968358
6954180 251 None 0 Human Functional pEC50 None 5.7 5.7 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@@H]1C[NH+]2CCC1CC2 8968358
20824 220186 None 0 Human Functional pIC50 = 8.3 8.3 1 2
NoneNone
Drug Central 378 5 3 5 0.5 CC1(C)S[C@@H]2[C@H](NC(=O)C(C(O)=O)C3=CC=CC=C3)C(=O)N2[C@H]1C(O)=O None
18381 220193 None 0 Human Functional pIC50 = 8.3 8.3 -1 4
NoneNone
Drug Central 469 4 2 6 3.2 CC1=C(C(=O)N[C@H]2[C@H]3SC(C)(C)[C@@H](N3C2=O)C(O)=O)C(=NO1)C1=C(Cl)C=CC=C1Cl None
11693 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
11693 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
3494 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
3494 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
3494.0 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
3494.0 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
4302 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
4302 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
7459 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
7459 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
9933193 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
9933193 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
9933193.0 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
9933193.0 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
CHEMBL1201335 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
CHEMBL1201335 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
DB00986 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
DB00986 1827 None 12 Human Functional pIC50 = 9.7 9.7 1 7
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
154059 3637 None 37 Human Functional pIC50 = 6.9 6.9 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
154059.0 3637 None 37 Human Functional pIC50 = 6.9 6.9 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
2457 3637 None 37 Human Functional pIC50 = 6.9 6.9 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
7483 3637 None 37 Human Functional pIC50 = 6.9 6.9 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
CHEMBL1734 3637 None 37 Human Functional pIC50 = 6.9 6.9 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
DB01591 3637 None 37 Human Functional pIC50 = 6.9 6.9 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
6433090 220228 None 0 Human Functional pKb = 8.0 8.0 -1 2
NoneNone
Drug Central 319 6 1 3 3.1 CC1=NC=CN1CCC(C(N)=O)(C1=CC=CC=C1)C1=CC=CC=C1 None
6433090.0 220228 None 0 Human Functional pKb = 8.0 8.0 -1 2
NoneNone
Drug Central 319 6 1 3 3.1 CC1=NC=CN1CCC(C(N)=O)(C1=CC=CC=C1)C1=CC=CC=C1 None
CHEMBL53366 220228 None 0 Human Functional pKb = 8.0 8.0 -1 2
NoneNone
Drug Central 319 6 1 3 3.1 CC1=NC=CN1CCC(C(N)=O)(C1=CC=CC=C1)C1=CC=CC=C1 None
DB09262 220228 None 0 Human Functional pKb = 8.0 8.0 -1 2
NoneNone
Drug Central 319 6 1 3 3.1 CC1=NC=CN1CCC(C(N)=O)(C1=CC=CC=C1)C1=CC=CC=C1 None




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367 3824 None 10 Human Binding pAC50 = 9.4 9.4 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
5487427 3824 None 10 Human Binding pAC50 = 9.4 9.4 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
5487427.0 3824 None 10 Human Binding pAC50 = 9.4 9.4 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
8592 3824 None 10 Human Binding pAC50 = 9.4 9.4 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL1900528 3824 None 10 Human Binding pAC50 = 9.4 9.4 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL3305968 3824 None 10 Human Binding pAC50 = 9.4 9.4 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL4650755 3824 None 10 Human Binding pAC50 = 9.4 9.4 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
DB01409 3824 None 10 Human Binding pAC50 = 9.4 9.4 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
25897919 55668 None 12 Human Binding pAC50 = 8.8 8.8 -1 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
657308 55668 None 12 Human Binding pAC50 = 8.8 8.8 -1 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
657309 55668 None 12 Human Binding pAC50 = 8.8 8.8 -1 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL1621597 55668 None 12 Human Binding pAC50 = 8.8 8.8 -1 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
DB00332 55668 None 12 Human Binding pAC50 = 8.8 8.8 -1 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
11693 1827 None 12 Human Binding pAC50 = 8.7 8.7 -1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
3494 1827 None 12 Human Binding pAC50 = 8.7 8.7 -1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
3494.0 1827 None 12 Human Binding pAC50 = 8.7 8.7 -1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
4302 1827 None 12 Human Binding pAC50 = 8.7 8.7 -1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
7459 1827 None 12 Human Binding pAC50 = 8.7 8.7 -1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
9933193 1827 None 12 Human Binding pAC50 = 8.7 8.7 -1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
9933193.0 1827 None 12 Human Binding pAC50 = 8.7 8.7 -1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
CHEMBL1201335 1827 None 12 Human Binding pAC50 = 8.7 8.7 -1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
DB00986 1827 None 12 Human Binding pAC50 = 8.7 8.7 -1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
2784 952 None 9 Human Binding pAC50 = 8.7 8.7 -6 3
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
2784.0 952 None 9 Human Binding pAC50 = 8.7 8.7 -6 3
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
351 952 None 9 Human Binding pAC50 = 8.7 8.7 -6 3
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
366 952 None 9 Human Binding pAC50 = 8.7 8.7 -6 3
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
676 952 None 9 Human Binding pAC50 = 8.7 8.7 -6 3
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL620 952 None 9 Human Binding pAC50 = 8.7 8.7 -6 3
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
DB00771 952 None 9 Human Binding pAC50 = 8.7 8.7 -6 3
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
3000322 3562 None 29 Human Binding pAC50 = 8.7 8.7 -2 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
3000322.0 3562 None 29 Human Binding pAC50 = 8.7 8.7 -2 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
330 3562 None 29 Human Binding pAC50 = 8.7 8.7 -2 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
CHEMBL569713 3562 None 29 Human Binding pAC50 = 8.7 8.7 -2 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
DB00747 3562 None 29 Human Binding pAC50 = 8.7 8.7 -2 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
2247 505 None 55 Human Binding pAC50 = 5 5.0 -19 41
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 None 55 Human Binding pAC50 = 5 5.0 -19 41
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 None 55 Human Binding pAC50 = 5 5.0 -19 41
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 None 55 Human Binding pAC50 = 5 5.0 -19 41
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 None 55 Human Binding pAC50 = 5 5.0 -19 41
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
3658 4107 None 38 Human Binding pAC50 = 5 5.0 - 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
517 4107 None 38 Human Binding pAC50 = 5 5.0 - 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709 4107 None 38 Human Binding pAC50 = 5 5.0 - 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709.0 4107 None 38 Human Binding pAC50 = 5 5.0 - 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL312448 4107 None 38 Human Binding pAC50 = 5 5.0 - 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
DB06694 4107 None 38 Human Binding pAC50 = 5 5.0 - 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
135398735 137055 None 20 Human Binding pAC50 = 5 5.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
136262914 137055 None 20 Human Binding pAC50 = 5 5.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL374478 137055 None 20 Human Binding pAC50 = 5 5.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
2136 3095 None 24 Human Binding pAC50 = 5.0 5.0 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
4768 3095 None 24 Human Binding pAC50 = 5.0 5.0 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
4768.0 3095 None 24 Human Binding pAC50 = 5.0 5.0 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
7268 3095 None 24 Human Binding pAC50 = 5.0 5.0 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL753 3095 None 24 Human Binding pAC50 = 5.0 5.0 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
DB00925 3095 None 24 Human Binding pAC50 = 5.0 5.0 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
5318 15583 None 40 Human Binding pAC50 = 5.0 5.0 -1 13
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1200348 15583 None 40 Human Binding pAC50 = 5.0 5.0 -1 13
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1221 15583 None 40 Human Binding pAC50 = 5.0 5.0 -1 13
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
216416 111644 None 40 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 111644 None 40 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
68617 207985 None 33 Human Binding pAC50 = 5.0 5.0 -12 25
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 207985 None 33 Human Binding pAC50 = 5.0 5.0 -12 25
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 207985 None 33 Human Binding pAC50 = 5.0 5.0 -12 25
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
2131 57423 None 16 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 536 14 2 2 4.6 CC[N+](CC)(CCNC(=O)C(=O)NCC[N+](CC)(CC)Cc1ccccc1Cl)Cc1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1652 57423 None 16 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 536 14 2 2 4.6 CC[N+](CC)(CCNC(=O)C(=O)NCC[N+](CC)(CC)Cc1ccccc1Cl)Cc1ccccc1Cl 10.1038/s41467-023-40064-9
23480 124157 None 21 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 5 1 1 5.0 CC(CC(c1ccccc1)c1ccccc1)NC(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL363295 124157 None 21 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 5 1 1 5.0 CC(CC(c1ccccc1)c1ccccc1)NC(C)(C)C 10.1038/s41467-023-40064-9
3042 1414 None 26 Human Binding pAC50 = 6.9 6.9 -1 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
3042.0 1414 None 26 Human Binding pAC50 = 6.9 6.9 -1 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
355 1414 None 26 Human Binding pAC50 = 6.9 6.9 -1 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
868 1414 None 26 Human Binding pAC50 = 6.9 6.9 -1 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
CHEMBL1123 1414 None 26 Human Binding pAC50 = 6.9 6.9 -1 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
DB00804 1414 None 26 Human Binding pAC50 = 6.9 6.9 -1 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
26987 949 None 27 Human Binding pAC50 = 5.9 5.9 -56 21
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
26987.0 949 None 27 Human Binding pAC50 = 5.9 5.9 -56 21
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
6063 949 None 27 Human Binding pAC50 = 5.9 5.9 -56 21
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
671 949 None 27 Human Binding pAC50 = 5.9 5.9 -56 21
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL1626 949 None 27 Human Binding pAC50 = 5.9 5.9 -56 21
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
DB00283 949 None 27 Human Binding pAC50 = 5.9 5.9 -56 21
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
2284 3182 None 26 Human Binding pAC50 = 5.9 5.9 -10 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 3182 None 26 Human Binding pAC50 = 5.9 5.9 -10 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 3182 None 26 Human Binding pAC50 = 5.9 5.9 -10 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 3182 None 26 Human Binding pAC50 = 5.9 5.9 -10 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 3182 None 26 Human Binding pAC50 = 5.9 5.9 -10 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
16363 596 None 33 Human Binding pAC50 = 4.9 4.9 - 6
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
16363.0 596 None 33 Human Binding pAC50 = 4.9 4.9 - 6
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
312 596 None 33 Human Binding pAC50 = 4.9 4.9 - 6
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
9215 596 None 33 Human Binding pAC50 = 4.9 4.9 - 6
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL297302 596 None 33 Human Binding pAC50 = 4.9 4.9 - 6
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB12867 596 None 33 Human Binding pAC50 = 4.9 4.9 - 6
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2274 3173 None 38 Human Binding pAC50 = 4.9 4.9 -21 32
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917 3173 None 38 Human Binding pAC50 = 4.9 4.9 -21 32
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917.0 3173 None 38 Human Binding pAC50 = 4.9 4.9 -21 32
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
7279 3173 None 38 Human Binding pAC50 = 4.9 4.9 -21 32
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL728 3173 None 38 Human Binding pAC50 = 4.9 4.9 -21 32
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00433 3173 None 38 Human Binding pAC50 = 4.9 4.9 -21 32
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2448 99377 None 50 Human Binding pAC50 = 4.9 4.9 -134 17
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
2448.0 99377 None 50 Human Binding pAC50 = 4.9 4.9 -134 17
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL28218 99377 None 50 Human Binding pAC50 = 4.9 4.9 -134 17
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
DB12401 99377 None 50 Human Binding pAC50 = 4.9 4.9 -134 17
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
135564886 14499 None 5 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
135673376 14499 None 5 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
137157436 14499 None 5 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
145948239 14499 None 5 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
71587099 14499 None 5 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
CHEMBL1201304 14499 None 5 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
41684 31229 None 62 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 31229 None 62 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
30323 62505 None 35 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL1563 62505 None 35 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL178 62505 None 35 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
68867 78202 None 29 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
68867.0 78202 None 29 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL2104523 78202 None 29 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
DB08810 78202 None 29 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
3926 209699 None 30 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL92870 209699 None 30 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
4919 208692 None 16 Human Binding pAC50 = 6.9 6.9 -2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
4919.0 208692 None 16 Human Binding pAC50 = 6.9 6.9 -2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL86715 208692 None 16 Human Binding pAC50 = 6.9 6.9 -2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
DB00387 208692 None 16 Human Binding pAC50 = 6.9 6.9 -2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
3121 7887 None 64 Human Binding pAC50 = 5.9 5.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 144 5 1 1 2.3 CCCC(CCC)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL109 7887 None 64 Human Binding pAC50 = 5.9 5.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 144 5 1 1 2.3 CCCC(CCC)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL433 7887 None 64 Human Binding pAC50 = 5.9 5.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 144 5 1 1 2.3 CCCC(CCC)C(=O)O 10.1038/s41467-023-40064-9
2540 4402 None 68 Human Binding pAC50 = 4.9 4.9 - 4
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
CHEMBL1014 4402 None 68 Human Binding pAC50 = 4.9 4.9 - 4
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
1613 2348 None 42 Human Binding pAC50 = 5.9 5.9 -15 44
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2348 None 42 Human Binding pAC50 = 5.9 5.9 -15 44
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2348 None 42 Human Binding pAC50 = 5.9 5.9 -15 44
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964.0 2348 None 42 Human Binding pAC50 = 5.9 5.9 -15 44
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2348 None 42 Human Binding pAC50 = 5.9 5.9 -15 44
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2348 None 42 Human Binding pAC50 = 5.9 5.9 -15 44
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
21772 78430 None 26 Human Binding pAC50 = 5.9 5.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 293 4 0 1 4.5 CC(CC1c2ccccc2CCc2ccccc21)CN(C)C 10.1038/s41467-023-40064-9
CHEMBL2110816 78430 None 26 Human Binding pAC50 = 5.9 5.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 293 4 0 1 4.5 CC(CC1c2ccccc2CCc2ccccc21)CN(C)C 10.1038/s41467-023-40064-9
156419 938 None 48 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
156419.0 938 None 48 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3308 938 None 48 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
647 938 None 48 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL1201284 938 None 48 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB01012 938 None 48 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
42890 9427 None 34 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
CHEMBL1117 9427 None 34 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
4011 82440 None 34 Human Binding pAC50 = 5.8 5.8 -14 23
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
CHEMBL21731 82440 None 34 Human Binding pAC50 = 5.8 5.8 -14 23
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
4413 98126 None 43 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
CHEMBL273264 98126 None 43 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
2726 919 None 48 Human Binding pAC50 = 5.8 5.8 -18 72
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2726.0 919 None 48 Human Binding pAC50 = 5.8 5.8 -18 72
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 919 None 48 Human Binding pAC50 = 5.8 5.8 -18 72
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 919 None 48 Human Binding pAC50 = 5.8 5.8 -18 72
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 919 None 48 Human Binding pAC50 = 5.8 5.8 -18 72
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 919 None 48 Human Binding pAC50 = 5.8 5.8 -18 72
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
10100 15300 None 4 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 339 8 0 3 4.3 CCC(=O)O[C@](Cc1ccccc1)(c1ccccc1)[C@H](C)CN(C)C 10.1038/s41467-023-40064-9
CHEMBL1213351 15300 None 4 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 339 8 0 3 4.3 CCC(=O)O[C@](Cc1ccccc1)(c1ccccc1)[C@H](C)CN(C)C 10.1038/s41467-023-40064-9
1549120 198942 None 55 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 319 4 1 4 2.9 CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL56337 198942 None 55 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 319 4 1 4 2.9 CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1 10.1038/s41467-023-40064-9
5329102 194838 None 50 Human Binding pAC50 = 5.8 5.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194838 None 50 Human Binding pAC50 = 5.8 5.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
2398 954 None 43 Human Binding pAC50 = 5.8 5.8 -1 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 954 None 43 Human Binding pAC50 = 5.8 5.8 -1 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801.0 954 None 43 Human Binding pAC50 = 5.8 5.8 -1 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 954 None 43 Human Binding pAC50 = 5.8 5.8 -1 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 954 None 43 Human Binding pAC50 = 5.8 5.8 -1 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 954 None 43 Human Binding pAC50 = 5.8 5.8 -1 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
1164 1630 None 10 Human Binding pAC50 = 5.8 5.8 - 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
1626 1630 None 10 Human Binding pAC50 = 5.8 5.8 - 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
3345 1630 None 10 Human Binding pAC50 = 5.8 5.8 - 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
3345.0 1630 None 10 Human Binding pAC50 = 5.8 5.8 - 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL596 1630 None 10 Human Binding pAC50 = 5.8 5.8 - 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
DB00813 1630 None 10 Human Binding pAC50 = 5.8 5.8 - 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
72093 35070 None 5 Human Binding pAC50 = 5.8 5.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 35070 None 5 Human Binding pAC50 = 5.8 5.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 35070 None 5 Human Binding pAC50 = 5.8 5.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
2351 4301 None 35 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 4301 None 35 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 4301 None 35 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
3826 178897 None 57 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 3 1 3 2.3 O=C(c1ccccc1)c1ccc2n1CCC2C(=O)O 10.1038/s41467-023-40064-9
CHEMBL469 178897 None 57 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 3 1 3 2.3 O=C(c1ccccc1)c1ccc2n1CCC2C(=O)O 10.1038/s41467-023-40064-9
8612 11264 None 26 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 270 6 1 4 2.4 CCN(CC)CCOC(=O)c1ccc(N)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL1179047 11264 None 26 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 270 6 1 4 2.4 CCN(CC)CCOC(=O)c1ccc(N)cc1Cl 10.1038/s41467-023-40064-9
9429 204590 None 44 Human Binding pAC50 = 4.8 4.8 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
9429.0 204590 None 44 Human Binding pAC50 = 4.8 4.8 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL609109 204590 None 44 Human Binding pAC50 = 4.8 4.8 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
DB01622 204590 None 44 Human Binding pAC50 = 4.8 4.8 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
319 1324 None 32 Human Binding pAC50 = 7.8 7.8 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
321 1324 None 32 Human Binding pAC50 = 7.8 7.8 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
444031 1324 None 32 Human Binding pAC50 = 7.8 7.8 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
444031.0 1324 None 32 Human Binding pAC50 = 7.8 7.8 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
784 1324 None 32 Human Binding pAC50 = 7.8 7.8 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
CHEMBL1346 1324 None 32 Human Binding pAC50 = 7.8 7.8 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
DB00496 1324 None 32 Human Binding pAC50 = 7.8 7.8 2 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
1530 2182 None 36 Human Binding pAC50 = 7.8 7.8 -147 24
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
3827 2182 None 36 Human Binding pAC50 = 7.8 7.8 -147 24
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
3827.0 2182 None 36 Human Binding pAC50 = 7.8 7.8 -147 24
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
7206 2182 None 36 Human Binding pAC50 = 7.8 7.8 -147 24
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
CHEMBL534 2182 None 36 Human Binding pAC50 = 7.8 7.8 -147 24
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
DB00920 2182 None 36 Human Binding pAC50 = 7.8 7.8 -147 24
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
4940 14476 None 26 Human Binding pAC50 = 6.8 6.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 340 5 0 4 4.8 CCC(=O)c1ccc2c(c1)N(CC(C)N(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1201210 14476 None 26 Human Binding pAC50 = 6.8 6.8 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 340 5 0 4 4.8 CCC(=O)c1ccc2c(c1)N(CC(C)N(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
1224 1432 None 51 Human Binding pAC50 = 5.8 5.8 -5 13
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 1432 None 51 Human Binding pAC50 = 5.8 5.8 -5 13
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100.0 1432 None 51 Human Binding pAC50 = 5.8 5.8 -5 13
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 1432 None 51 Human Binding pAC50 = 5.8 5.8 -5 13
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 1432 None 51 Human Binding pAC50 = 5.8 5.8 -5 13
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 1432 None 51 Human Binding pAC50 = 5.8 5.8 -5 13
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 1432 None 51 Human Binding pAC50 = 5.8 5.8 -5 13
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
5280453 208429 None 49 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 3 3 5.7 C=C1/C(=C\C=C2/CCC[C@]3(C)[C@@H]([C@H](C)CCCC(C)(C)O)CC[C@@H]23)C[C@@H](O)C[C@@H]1O 10.1038/s41467-023-40064-9
CHEMBL846 208429 None 49 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 3 3 5.7 C=C1/C(=C\C=C2/CCC[C@]3(C)[C@@H]([C@H](C)CCCC(C)(C)O)CC[C@@H]23)C[C@@H](O)C[C@@H]1O 10.1038/s41467-023-40064-9
1605 2342 None 72 Human Binding pAC50 = 4.7 4.7 - 4
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
3957 2342 None 72 Human Binding pAC50 = 4.7 4.7 - 4
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
3957.0 2342 None 72 Human Binding pAC50 = 4.7 4.7 - 4
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
7216 2342 None 72 Human Binding pAC50 = 4.7 4.7 - 4
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
CHEMBL998 2342 None 72 Human Binding pAC50 = 4.7 4.7 - 4
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
DB00455 2342 None 72 Human Binding pAC50 = 4.7 4.7 - 4
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 1 0 3 4.9 CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1 10.1038/s41467-023-40064-9
20628 96601 None 25 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
CHEMBL26291 96601 None 25 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
4832 55436 None 14 Human Binding pAC50 = 7.7 7.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 5 1 3 3.1 CC[N+]1(C)CCCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL1619528 55436 None 14 Human Binding pAC50 = 7.7 7.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 5 1 3 3.1 CC[N+]1(C)CCCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1038/s41467-023-40064-9
2705 3842 None 44 Human Binding pAC50 = 7.7 7.7 -1 11
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
360 3842 None 44 Human Binding pAC50 = 7.7 7.7 -1 11
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
443879 3842 None 44 Human Binding pAC50 = 7.7 7.7 -1 11
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
443879.0 3842 None 44 Human Binding pAC50 = 7.7 7.7 -1 11
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
CHEMBL1382 3842 None 44 Human Binding pAC50 = 7.7 7.7 -1 11
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
DB01036 3842 None 44 Human Binding pAC50 = 7.7 7.7 -1 11
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
6127 14505 None 4 Human Binding pAC50 = 6.7 6.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
6127.0 14505 None 4 Human Binding pAC50 = 6.7 6.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1201340 14505 None 4 Human Binding pAC50 = 6.7 6.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
DB13720 14505 None 4 Human Binding pAC50 = 6.7 6.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
135 2532 None 33 Human Binding pAC50 = 5.7 5.7 -22 57
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 2532 None 33 Human Binding pAC50 = 5.7 5.7 -22 57
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 2532 None 33 Human Binding pAC50 = 5.7 5.7 -22 57
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184.0 2532 None 33 Human Binding pAC50 = 5.7 5.7 -22 57
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 2532 None 33 Human Binding pAC50 = 5.7 5.7 -22 57
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 2532 None 33 Human Binding pAC50 = 5.7 5.7 -22 57
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
2200 3131 None 31 Human Binding pAC50 = 5.7 5.7 -7 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
328 3131 None 31 Human Binding pAC50 = 5.7 5.7 -7 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
4848 3131 None 31 Human Binding pAC50 = 5.7 5.7 -7 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
4848.0 3131 None 31 Human Binding pAC50 = 5.7 5.7 -7 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
CHEMBL9967 3131 None 31 Human Binding pAC50 = 5.7 5.7 -7 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
DB00670 3131 None 31 Human Binding pAC50 = 5.7 5.7 -7 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
11434515 261 None 6 Human Binding pAC50 = 8.6 8.6 -4 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
11434515.0 261 None 6 Human Binding pAC50 = 8.6 8.6 -4 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
11519741 261 None 6 Human Binding pAC50 = 8.6 8.6 -4 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
4484 261 None 6 Human Binding pAC50 = 8.6 8.6 -4 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
7449 261 None 6 Human Binding pAC50 = 8.6 8.6 -4 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL1194325 261 None 6 Human Binding pAC50 = 8.6 8.6 -4 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
DB08897 261 None 6 Human Binding pAC50 = 8.6 8.6 -4 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
16351 102785 None 36 Human Binding pAC50 = 5.7 5.7 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
16351.0 102785 None 36 Human Binding pAC50 = 5.7 5.7 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL304902 102785 None 36 Human Binding pAC50 = 5.7 5.7 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
DB13256 102785 None 36 Human Binding pAC50 = 5.7 5.7 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
1210 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1213 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
2725 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
33036 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
33036.0 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
4411 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
616 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
6976 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
716121 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1201353 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1554789 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL505 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB01114 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB13679 918 None 42 Human Binding pAC50 = 4.7 4.7 -125 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
47472 19444 None 41 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 410 7 0 3 6.6 Clc1ccc(CCC(Cn2ccnc2)Sc2c(Cl)cccc2Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1295 19444 None 41 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 410 7 0 3 6.6 Clc1ccc(CCC(Cn2ccnc2)Sc2c(Cl)cccc2Cl)cc1 10.1038/s41467-023-40064-9
51755 57422 None 40 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 454 8 0 4 7.3 Clc1ccc(C(Cn2ccnc2)OCc2ccc(Sc3ccccc3)cc2)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1651990 57422 None 40 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 454 8 0 4 7.3 Clc1ccc(C(Cn2ccnc2)OCc2ccc(Sc3ccccc3)cc2)c(Cl)c1 10.1038/s41467-023-40064-9
60753 194796 None 31 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 384 14 2 4 4.2 CCCCCCCN(CC)CCCC(O)c1ccc(NS(C)(=O)=O)cc1 10.1038/s41467-023-40064-9
CHEMBL533 194796 None 31 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 384 14 2 4 4.2 CCCCCCCN(CC)CCCC(O)c1ccc(NS(C)(=O)=O)cc1 10.1038/s41467-023-40064-9
2435 3590 None 59 Human Binding pAC50 = 4.7 4.7 -239 48
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 3590 None 59 Human Binding pAC50 = 4.7 4.7 -239 48
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 3590 None 59 Human Binding pAC50 = 4.7 4.7 -239 48
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 3590 None 59 Human Binding pAC50 = 4.7 4.7 -239 48
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 3590 None 59 Human Binding pAC50 = 4.7 4.7 -239 48
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
4846 27995 None 38 Human Binding pAC50 = 5.7 5.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 1 2 6 2.2 O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1 10.1038/s41467-023-40064-9
CHEMBL1372341 27995 None 38 Human Binding pAC50 = 5.7 5.7 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 1 2 6 2.2 O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1 10.1038/s41467-023-40064-9
3081361 93987 None 66 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
CHEMBL24828 93987 None 66 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
4976 206037 None 20 Human Binding pAC50 = 6.6 6.6 -1 11
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL668 206037 None 20 Human Binding pAC50 = 6.6 6.6 -1 11
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
107771 120312 None 42 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
CHEMBL35228 120312 None 42 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
5482 14425 None 55 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1200438 14425 None 55 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
1201549 597 None 17 Human Binding pAC50 = 7.6 7.6 -1 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
1201549.0 597 None 17 Human Binding pAC50 = 7.6 7.6 -1 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
333 597 None 17 Human Binding pAC50 = 7.6 7.6 -1 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7601 597 None 17 Human Binding pAC50 = 7.6 7.6 -1 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201203 597 None 17 Human Binding pAC50 = 7.6 7.6 -1 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL438151 597 None 17 Human Binding pAC50 = 7.6 7.6 -1 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00245 597 None 17 Human Binding pAC50 = 7.6 7.6 -1 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
180 401 None 38 Human Binding pAC50 = 6.6 6.6 -23 39
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 401 None 38 Human Binding pAC50 = 6.6 6.6 -23 39
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 401 None 38 Human Binding pAC50 = 6.6 6.6 -23 39
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160.0 401 None 38 Human Binding pAC50 = 6.6 6.6 -23 39
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 401 None 38 Human Binding pAC50 = 6.6 6.6 -23 39
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 401 None 38 Human Binding pAC50 = 6.6 6.6 -23 39
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3191 102913 None 65 Human Binding pAC50 = 5.6 5.6 -6 25
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
3191.0 102913 None 65 Human Binding pAC50 = 5.6 5.6 -6 25
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL305660 102913 None 65 Human Binding pAC50 = 5.6 5.6 -6 25
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
DB11742 102913 None 65 Human Binding pAC50 = 5.6 5.6 -6 25
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
2318 154946 None 18 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL400599 154946 None 18 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
4452 2762 None 13 Human Binding pAC50 = 4.6 4.6 - 18
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
983 2762 None 13 Human Binding pAC50 = 4.6 4.6 - 18
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
CHEMBL20734 2762 None 13 Human Binding pAC50 = 4.6 4.6 - 18
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
6337614 13001 None 38 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 296 1 0 2 2.7 O=C1c2cccc3c2[C@H](CCC3)CN1[C@@H]1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL1189679 13001 None 38 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 296 1 0 2 2.7 O=C1c2cccc3c2[C@H](CCC3)CN1[C@@H]1CN2CCC1CC2 10.1038/s41467-023-40064-9
127151 35339 None 12 Human Binding pAC50 = 4.6 4.6 - 10
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 10.1038/s41467-023-40064-9
3022645 35339 None 12 Human Binding pAC50 = 4.6 4.6 - 10
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 10.1038/s41467-023-40064-9
CHEMBL14370 35339 None 12 Human Binding pAC50 = 4.6 4.6 - 10
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 10.1038/s41467-023-40064-9
CHEMBL2103737 78169 None 0 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
2995 206863 None 31 Human Binding pAC50 = 5.5 5.5 -5 22
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
2995.0 206863 None 31 Human Binding pAC50 = 5.5 5.5 -5 22
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1696 206863 None 31 Human Binding pAC50 = 5.5 5.5 -5 22
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL72 206863 None 31 Human Binding pAC50 = 5.5 5.5 -5 22
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
DB01151 206863 None 31 Human Binding pAC50 = 5.5 5.5 -5 22
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
656603 194645 None 3 Human Binding pAC50 = 8.5 8.5 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 6 1 3 3.6 C[N@+]1(CCF)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)(c1ccccc1)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL5292015 194645 None 3 Human Binding pAC50 = 8.5 8.5 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 6 1 3 3.6 C[N@+]1(CCF)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)(c1ccccc1)c1ccccc1)C2 10.1038/s41467-023-40064-9
191 403 None 60 Human Binding pAC50 = 5.5 5.5 -37 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 403 None 60 Human Binding pAC50 = 5.5 5.5 -37 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 403 None 60 Human Binding pAC50 = 5.5 5.5 -37 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170.0 403 None 60 Human Binding pAC50 = 5.5 5.5 -37 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 403 None 60 Human Binding pAC50 = 5.5 5.5 -37 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 403 None 60 Human Binding pAC50 = 5.5 5.5 -37 28
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
11980903 14498 None 13 Human Binding pAC50 = 5.5 5.5 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 14498 None 13 Human Binding pAC50 = 5.5 5.5 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 14498 None 13 Human Binding pAC50 = 5.5 5.5 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 14498 None 13 Human Binding pAC50 = 5.5 5.5 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
2286 3183 None 36 Human Binding pAC50 = 6.5 6.5 -2 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 3183 None 36 Human Binding pAC50 = 6.5 6.5 -2 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927.0 3183 None 36 Human Binding pAC50 = 6.5 6.5 -2 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 3183 None 36 Human Binding pAC50 = 6.5 6.5 -2 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 3183 None 36 Human Binding pAC50 = 6.5 6.5 -2 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 3183 None 36 Human Binding pAC50 = 6.5 6.5 -2 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
103 4153 None 44 Human Binding pAC50 = 5.5 5.5 -144 53
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 4153 None 44 Human Binding pAC50 = 5.5 5.5 -144 53
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 4153 None 44 Human Binding pAC50 = 5.5 5.5 -144 53
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 4153 None 44 Human Binding pAC50 = 5.5 5.5 -144 53
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 4153 None 44 Human Binding pAC50 = 5.5 5.5 -144 53
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2895 206050 None 27 Human Binding pAC50 = 6.5 6.5 -1 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
2895.0 206050 None 27 Human Binding pAC50 = 6.5 6.5 -1 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL669 206050 None 27 Human Binding pAC50 = 6.5 6.5 -1 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
DB00924 206050 None 27 Human Binding pAC50 = 6.5 6.5 -1 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
1385580 29284 None 49 Human Binding pAC50 = 5.5 5.5 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4615 29284 None 49 Human Binding pAC50 = 5.5 5.5 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4615.0 29284 None 49 Human Binding pAC50 = 5.5 5.5 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL13828 29284 None 49 Human Binding pAC50 = 5.5 5.5 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
DB12877 29284 None 49 Human Binding pAC50 = 5.5 5.5 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
657202 12534 None 3 Human Binding pAC50 = 7.4 7.4 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 282 6 0 2 3.5 CCCC(CCC)C(=O)O[C@H]1C[C@H]2CC[C@@H](C1)[N+]2(C)C 10.1038/s41467-023-40064-9
CHEMBL1186610 12534 None 3 Human Binding pAC50 = 7.4 7.4 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 282 6 0 2 3.5 CCCC(CCC)C(=O)O[C@H]1C[C@H]2CC[C@@H](C1)[N+]2(C)C 10.1038/s41467-023-40064-9
4756 16656 None 34 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
CHEMBL1201022 16656 None 34 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
CHEMBL1242 16656 None 34 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
135398745 2914 None 65 Human Binding pAC50 = 6.4 6.4 -27 65
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
135398745.0 2914 None 65 Human Binding pAC50 = 6.4 6.4 -27 65
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2914 None 65 Human Binding pAC50 = 6.4 6.4 -27 65
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2914 None 65 Human Binding pAC50 = 6.4 6.4 -27 65
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2914 None 65 Human Binding pAC50 = 6.4 6.4 -27 65
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
2774 3868 None 59 Human Binding pAC50 = 6.4 6.4 -2 10
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
5593 3868 None 59 Human Binding pAC50 = 6.4 6.4 -2 10
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
5593.0 3868 None 59 Human Binding pAC50 = 6.4 6.4 -2 10
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
7319 3868 None 59 Human Binding pAC50 = 6.4 6.4 -2 10
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
CHEMBL1200604 3868 None 59 Human Binding pAC50 = 6.4 6.4 -2 10
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
DB00809 3868 None 59 Human Binding pAC50 = 6.4 6.4 -2 10
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
DB01199 3868 None 59 Human Binding pAC50 = 6.4 6.4 -2 10
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
3158 56283 None 21 Human Binding pAC50 = 6.4 6.4 -104 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
3158.0 56283 None 21 Human Binding pAC50 = 6.4 6.4 -104 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56283 None 21 Human Binding pAC50 = 6.4 6.4 -104 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB01142 56283 None 21 Human Binding pAC50 = 6.4 6.4 -104 20
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
25382 9159 None 27 Human Binding pAC50 = 6.4 6.4 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL110094 9159 None 27 Human Binding pAC50 = 6.4 6.4 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
154417 23189 None 39 Human Binding pAC50 = 8.4 8.4 -1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL1331216 23189 None 39 Human Binding pAC50 = 8.4 8.4 -1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
2905 14504 None 36 Human Binding pAC50 = 7.4 7.4 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 10.1038/s41467-023-40064-9
2905.0 14504 None 36 Human Binding pAC50 = 7.4 7.4 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 10.1038/s41467-023-40064-9
CHEMBL1201338 14504 None 36 Human Binding pAC50 = 7.4 7.4 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 10.1038/s41467-023-40064-9
DB00979 14504 None 36 Human Binding pAC50 = 7.4 7.4 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 10.1038/s41467-023-40064-9
5284550 41735 None 12 Human Binding pAC50 = 6.4 6.4 -1 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
5284550.0 41735 None 12 Human Binding pAC50 = 6.4 6.4 -1 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL108947 41735 None 12 Human Binding pAC50 = 6.4 6.4 -1 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1492500 41735 None 12 Human Binding pAC50 = 6.4 6.4 -1 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
DB09167 41735 None 12 Human Binding pAC50 = 6.4 6.4 -1 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
2335 11852 None 18 Human Binding pAC50 = 5.4 5.4 -1 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 11852 None 18 Human Binding pAC50 = 5.4 5.4 -1 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 11852 None 18 Human Binding pAC50 = 5.4 5.4 -1 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 11852 None 18 Human Binding pAC50 = 5.4 5.4 -1 12
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
43815 187026 None 38 Human Binding pAC50 = 6.4 6.4 -5 24
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL1708 187026 None 38 Human Binding pAC50 = 6.4 6.4 -5 24
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL490 187026 None 38 Human Binding pAC50 = 6.4 6.4 -5 24
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
3947 208853 None 39 Human Binding pAC50 = 5.3 5.3 -4 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL87708 208853 None 39 Human Binding pAC50 = 5.3 5.3 -4 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
3775 14481 None 19 Human Binding pAC50 = 8.3 8.3 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 353 8 1 1 4.1 CC(C)[N+](C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
3775.0 14481 None 19 Human Binding pAC50 = 8.3 8.3 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 353 8 1 1 4.1 CC(C)[N+](C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
CHEMBL1201232 14481 None 19 Human Binding pAC50 = 8.3 8.3 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 353 8 1 1 4.1 CC(C)[N+](C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
DB01625 14481 None 19 Human Binding pAC50 = 8.3 8.3 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 353 8 1 1 4.1 CC(C)[N+](C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
135398737 958 None 57 Human Binding pAC50 = 6.3 6.3 -10 91
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
135398737.0 958 None 57 Human Binding pAC50 = 6.3 6.3 -10 91
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 958 None 57 Human Binding pAC50 = 6.3 6.3 -10 91
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 958 None 57 Human Binding pAC50 = 6.3 6.3 -10 91
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 958 None 57 Human Binding pAC50 = 6.3 6.3 -10 91
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 958 None 57 Human Binding pAC50 = 6.3 6.3 -10 91
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
3394 198891 None 76 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 3 1 1 3.7 CC(C(=O)O)c1ccc(-c2ccccc2)c(F)c1 10.1038/s41467-023-40064-9
CHEMBL563 198891 None 76 Human Binding pAC50 = 6.3 6.3 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 3 1 1 3.7 CC(C(=O)O)c1ccc(-c2ccccc2)c(F)c1 10.1038/s41467-023-40064-9
260 3869 None 33 Human Binding pAC50 = 5.3 5.3 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2775 3869 None 33 Human Binding pAC50 = 5.3 5.3 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
656665 3869 None 33 Human Binding pAC50 = 5.3 5.3 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL56564 3869 None 33 Human Binding pAC50 = 5.3 5.3 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB11699 3869 None 33 Human Binding pAC50 = 5.3 5.3 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
1971 2866 None 32 Human Binding pAC50 = 6.3 6.3 -3 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 2866 None 32 Human Binding pAC50 = 6.3 6.3 -3 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 2866 None 32 Human Binding pAC50 = 6.3 6.3 -3 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543.0 2866 None 32 Human Binding pAC50 = 6.3 6.3 -3 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 2866 None 32 Human Binding pAC50 = 6.3 6.3 -3 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 2866 None 32 Human Binding pAC50 = 6.3 6.3 -3 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
19003 14416 None 24 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 3 3 5 0.3 CC1(C)S[C@@H]2[C@H](NC(=O)C3(N)CCCCC3)C(=O)N2[C@H]1C(=O)O 10.1038/s41467-023-40064-9
CHEMBL1200356 14416 None 24 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 3 3 5 0.3 CC1(C)S[C@@H]2[C@H](NC(=O)C3(N)CCCCC3)C(=O)N2[C@H]1C(=O)O 10.1038/s41467-023-40064-9
16722836 18992 None 63 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 524 10 3 8 4.8 Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1 10.1038/s41467-023-40064-9
CHEMBL1287853 18992 None 63 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 524 10 3 8 4.8 Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1 10.1038/s41467-023-40064-9
4031 99367 None 27 Human Binding pAC50 = 6.2 6.2 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 429 13 0 6 4.6 CCN(CCCCOC(=O)c1ccc(OC)c(OC)c1)C(C)Cc1ccc(OC)cc1 10.1038/s41467-023-40064-9
CHEMBL282121 99367 None 27 Human Binding pAC50 = 6.2 6.2 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 429 13 0 6 4.6 CCN(CCCCOC(=O)c1ccc(OC)c(OC)c1)C(C)Cc1ccc(OC)cc1 10.1038/s41467-023-40064-9
1209 1658 None 52 Human Binding pAC50 = 5.2 5.2 -30 31
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
203 1658 None 52 Human Binding pAC50 = 5.2 5.2 -30 31
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3386 1658 None 52 Human Binding pAC50 = 5.2 5.2 -30 31
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL41 1658 None 52 Human Binding pAC50 = 5.2 5.2 -30 31
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
DB00472 1658 None 52 Human Binding pAC50 = 5.2 5.2 -30 31
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
10096344 89628 None 56 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 10 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C 10.1038/s41467-023-40064-9
CHEMBL237500 89628 None 56 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 10 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C 10.1038/s41467-023-40064-9
3236 67630 None 28 Human Binding pAC50 = 5.2 5.2 - 2
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 259 5 0 2 3.6 CCc1ccc(C(=O)C(C)CN2CCCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1902981 67630 None 28 Human Binding pAC50 = 5.2 5.2 - 2
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 259 5 0 2 3.6 CCc1ccc(C(=O)C(C)CN2CCCCC2)cc1 10.1038/s41467-023-40064-9
3000322 3562 None 29 Human Binding pAC50 = 8.1 8.1 -2 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
3000322.0 3562 None 29 Human Binding pAC50 = 8.1 8.1 -2 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
330 3562 None 29 Human Binding pAC50 = 8.1 8.1 -2 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
CHEMBL569713 3562 None 29 Human Binding pAC50 = 8.1 8.1 -2 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
DB00747 3562 None 29 Human Binding pAC50 = 8.1 8.1 -2 8
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
21722 17999 None 26 Human Binding pAC50 = 5.1 5.1 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 17999 None 26 Human Binding pAC50 = 5.1 5.1 - 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
19910 37419 None 62 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 190 1 1 4 1.8 O=[N+]([O-])c1ccc(O)c2ncccc12 10.1038/s41467-023-40064-9
CHEMBL1454910 37419 None 62 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 190 1 1 4 1.8 O=[N+]([O-])c1ccc(O)c2ncccc12 10.1038/s41467-023-40064-9
124087 1389 None 72 Human Binding pAC50 = 6.1 6.1 -9 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
124087.0 1389 None 72 Human Binding pAC50 = 6.1 6.1 -9 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 1389 None 72 Human Binding pAC50 = 6.1 6.1 -9 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 1389 None 72 Human Binding pAC50 = 6.1 6.1 -9 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 1389 None 72 Human Binding pAC50 = 6.1 6.1 -9 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 1389 None 72 Human Binding pAC50 = 6.1 6.1 -9 15
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
214 3860 None 43 Human Binding pAC50 = 5.1 5.1 -93 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 3860 None 43 Human Binding pAC50 = 5.1 5.1 -93 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 3860 None 43 Human Binding pAC50 = 5.1 5.1 -93 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566.0 3860 None 43 Human Binding pAC50 = 5.1 5.1 -93 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 3860 None 43 Human Binding pAC50 = 5.1 5.1 -93 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 3860 None 43 Human Binding pAC50 = 5.1 5.1 -93 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 3860 None 43 Human Binding pAC50 = 5.1 5.1 -93 29
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3074 17965 None 17 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 604 16 0 12 3.5 COc1cc(C(=O)OCCCN2CCCN(CCCOC(=O)c3cc(OC)c(OC)c(OC)c3)CC2)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL126075 17965 None 17 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 604 16 0 12 3.5 COc1cc(C(=O)OCCCN2CCCN(CCCOC(=O)c3cc(OC)c(OC)c(OC)c3)CC2)cc(OC)c1OC 10.1038/s41467-023-40064-9
2713 207729 None 57 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 207729 None 57 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 207729 None 57 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 207729 None 57 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 207729 None 57 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1330113 207729 None 57 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 207729 None 57 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
1427 2013 None 42 Human Binding pAC50 = 6.1 6.1 -2 26
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2013 None 42 Human Binding pAC50 = 6.1 6.1 -2 26
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2013 None 42 Human Binding pAC50 = 6.1 6.1 -2 26
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2013 None 42 Human Binding pAC50 = 6.1 6.1 -2 26
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2013 None 42 Human Binding pAC50 = 6.1 6.1 -2 26
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
5284632 67423 None 10 Human Binding pAC50 = 8.1 8.1 1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
5284632.0 67423 None 10 Human Binding pAC50 = 8.1 8.1 1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1888176 67423 None 10 Human Binding pAC50 = 8.1 8.1 1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL3084748 67423 None 10 Human Binding pAC50 = 8.1 8.1 1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00209 67423 None 10 Human Binding pAC50 = 8.1 8.1 1 5
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
4450 178333 None 41 Human Binding pAC50 = 5.1 5.1 - 3
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 253 1 0 2 3.2 CN1CCOC(c2ccccc2)c2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL465026 178333 None 41 Human Binding pAC50 = 5.1 5.1 - 3
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 253 1 0 2 3.2 CN1CCOC(c2ccccc2)c2ccccc2C1 10.1038/s41467-023-40064-9
1222 1664 None 37 Human Binding pAC50 = 5.1 5.1 - 32
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396 1664 None 37 Human Binding pAC50 = 5.1 5.1 - 32
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396.0 1664 None 37 Human Binding pAC50 = 5.1 5.1 - 32
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
85 1664 None 37 Human Binding pAC50 = 5.1 5.1 - 32
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL46516 1664 None 37 Human Binding pAC50 = 5.1 5.1 - 32
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
DB04842 1664 None 37 Human Binding pAC50 = 5.1 5.1 - 32
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
4942 5720 None 27 Human Binding pAC50 = 6.1 6.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
4942.0 5720 None 27 Human Binding pAC50 = 6.1 6.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1078261 5720 None 27 Human Binding pAC50 = 6.1 6.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB12278 5720 None 27 Human Binding pAC50 = 6.1 6.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
3149 12618 None 11 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 12618 None 11 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
100 3805 None 44 Human Binding pAC50 = 6.1 6.1 -8 55
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 3805 None 44 Human Binding pAC50 = 6.1 6.1 -8 55
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 3805 None 44 Human Binding pAC50 = 6.1 6.1 -8 55
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 3805 None 44 Human Binding pAC50 = 6.1 6.1 -8 55
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 3805 None 44 Human Binding pAC50 = 6.1 6.1 -8 55
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5330286 67592 None 57 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 5 2 9 3.0 CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O 10.1038/s41467-023-40064-9
CHEMBL189963 67592 None 57 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 5 2 9 3.0 CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O 10.1038/s41467-023-40064-9
2337 3256 None 51 Human Binding pAC50 = 5.1 5.1 -81 62
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 3256 None 51 Human Binding pAC50 = 5.1 5.1 -81 62
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 3256 None 51 Human Binding pAC50 = 5.1 5.1 -81 62
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002.0 3256 None 51 Human Binding pAC50 = 5.1 5.1 -81 62
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 3256 None 51 Human Binding pAC50 = 5.1 5.1 -81 62
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 3256 None 51 Human Binding pAC50 = 5.1 5.1 -81 62
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5039 63203 None 12 Human Binding pAC50 = 5.1 5.1 - 1
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1038/s41467-023-40064-9
5039.0 63203 None 12 Human Binding pAC50 = 5.1 5.1 - 1
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1038/s41467-023-40064-9
CHEMBL1790041 63203 None 12 Human Binding pAC50 = 5.1 5.1 - 1
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1038/s41467-023-40064-9
DB00863 63203 None 12 Human Binding pAC50 = 5.1 5.1 - 1
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1038/s41467-023-40064-9
2179 167616 None 49 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL1256655 167616 None 49 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL43 167616 None 49 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
4066 207084 None 54 Human Binding pAC50 = 7.1 7.1 -1 7
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
4066.0 207084 None 54 Human Binding pAC50 = 7.1 7.1 -1 7
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL73451 207084 None 54 Human Binding pAC50 = 7.1 7.1 -1 7
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
DB01071 207084 None 54 Human Binding pAC50 = 7.1 7.1 -1 7
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
50922675 112647 None 47 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 539 9 3 9 3.9 COC(=O)N[C@@H](C)CNc1nccc(-c2cn(C(C)C)nc2-c2cc(Cl)cc(NS(C)(=O)=O)c2F)n1 10.1038/s41467-023-40064-9
CHEMBL3301612 112647 None 47 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 539 9 3 9 3.9 COC(=O)N[C@@H](C)CNc1nccc(-c2cn(C(C)C)nc2-c2cc(Cl)cc(NS(C)(=O)=O)c2F)n1 10.1038/s41467-023-40064-9
2381 663 None 30 Human Binding pAC50 = 6.1 6.1 -9 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
2381.0 663 None 30 Human Binding pAC50 = 6.1 6.1 -9 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
374 663 None 30 Human Binding pAC50 = 6.1 6.1 -9 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
7128 663 None 30 Human Binding pAC50 = 6.1 6.1 -9 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL1101 663 None 30 Human Binding pAC50 = 6.1 6.1 -9 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
DB00810 663 None 30 Human Binding pAC50 = 6.1 6.1 -9 9
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
1193 1656 None 64 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
2447 1656 None 64 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3371 1656 None 64 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL23588 1656 None 64 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB02266 1656 None 64 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
5453 206077 None 58 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
CHEMBL671 206077 None 58 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
19675 51685 None 37 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 410 7 1 5 5.0 CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1584 51685 None 37 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 410 7 1 5 5.0 CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
23724781 2835 None 13 Rat Binding pEC50 = 10.3 10.3 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
23724781.0 2835 None 13 Rat Binding pEC50 = 10.3 10.3 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
316 2835 None 13 Rat Binding pEC50 = 10.3 10.3 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
317 2835 None 13 Rat Binding pEC50 = 10.3 10.3 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
71183 2835 None 13 Rat Binding pEC50 = 10.3 10.3 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL1354199 2835 None 13 Rat Binding pEC50 = 10.3 10.3 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL3140030 2835 None 13 Rat Binding pEC50 = 10.3 10.3 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL376897 2835 None 13 Rat Binding pEC50 = 10.3 10.3 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
DB00462 2835 None 13 Rat Binding pEC50 = 10.3 10.3 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
23724781 2835 None 13 Rat Binding pEC50 = 9.7 9.7 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
23724781.0 2835 None 13 Rat Binding pEC50 = 9.7 9.7 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
316 2835 None 13 Rat Binding pEC50 = 9.7 9.7 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
317 2835 None 13 Rat Binding pEC50 = 9.7 9.7 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
71183 2835 None 13 Rat Binding pEC50 = 9.7 9.7 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL1354199 2835 None 13 Rat Binding pEC50 = 9.7 9.7 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL3140030 2835 None 13 Rat Binding pEC50 = 9.7 9.7 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL376897 2835 None 13 Rat Binding pEC50 = 9.7 9.7 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
DB00462 2835 None 13 Rat Binding pEC50 = 9.7 9.7 1 9
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
367 3824 None 10 Human Binding pEC50 = 9.4 9.4 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
5487427 3824 None 10 Human Binding pEC50 = 9.4 9.4 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
5487427.0 3824 None 10 Human Binding pEC50 = 9.4 9.4 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
8592 3824 None 10 Human Binding pEC50 = 9.4 9.4 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL1900528 3824 None 10 Human Binding pEC50 = 9.4 9.4 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL3305968 3824 None 10 Human Binding pEC50 = 9.4 9.4 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL4650755 3824 None 10 Human Binding pEC50 = 9.4 9.4 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
DB01409 3824 None 10 Human Binding pEC50 = 9.4 9.4 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
2230 465 None 43 Human Binding pEC50 = 7 7.0 -588 10
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00156a018
296 465 None 43 Human Binding pEC50 = 7 7.0 -588 10
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00156a018
CHEMBL7303 465 None 43 Human Binding pEC50 = 7 7.0 -588 10
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00156a018
DB04365 465 None 43 Human Binding pEC50 = 7 7.0 -588 10
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00156a018
9308 17761 None 16 Human Binding pEC50 = 6 6.0 - 7
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
CHEMBL1255785 17761 None 16 Human Binding pEC50 = 6 6.0 - 7
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
CHEMBL12587 17761 None 16 Human Binding pEC50 = 6 6.0 - 7
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
CHEMBL292911 17761 None 16 Human Binding pEC50 = 6 6.0 - 7
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
170332 161070 None 0 Human Binding pEC50 = 5 5.0 -7 3
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4091934 161070 None 0 Human Binding pEC50 = 5 5.0 -7 3
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115997 161070 None 0 Human Binding pEC50 = 5 5.0 -7 3
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
91468 209522 None 10 Human Binding pEC50 = 5.0 5.0 - 0
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
CHEMBL91776 209522 None 10 Human Binding pEC50 = 5.0 5.0 - 0
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
170332 161070 None 0 Human Binding pEC50 = 5.0 5.0 -7 3
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4091934 161070 None 0 Human Binding pEC50 = 5.0 5.0 -7 3
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115997 161070 None 0 Human Binding pEC50 = 5.0 5.0 -7 3
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
319 1324 None 32 Human Binding pEC50 = 8.0 8.0 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
321 1324 None 32 Human Binding pEC50 = 8.0 8.0 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031 1324 None 32 Human Binding pEC50 = 8.0 8.0 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031.0 1324 None 32 Human Binding pEC50 = 8.0 8.0 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
784 1324 None 32 Human Binding pEC50 = 8.0 8.0 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
CHEMBL1346 1324 None 32 Human Binding pEC50 = 8.0 8.0 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
DB00496 1324 None 32 Human Binding pEC50 = 8.0 8.0 2 9
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
13621561 11075 None 1 Human Binding pEC50 = 5.9 5.9 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 178 2 1 4 0.3 C#CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1177918 11075 None 1 Human Binding pEC50 = 5.9 5.9 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 178 2 1 4 0.3 C#CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL6767 11075 None 1 Human Binding pEC50 = 5.9 5.9 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 178 2 1 4 0.3 C#CCOc1noc2c1CNCC2 10.1021/jm00156a018
10261985 206407 None 0 Human Binding pEC50 = 6.9 6.9 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL69306 206407 None 0 Human Binding pEC50 = 6.9 6.9 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
13621555 11948 None 1 Human Binding pEC50 = 4.9 4.9 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 180 3 1 4 0.9 C=CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1182820 11948 None 1 Human Binding pEC50 = 4.9 4.9 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 180 3 1 4 0.9 C=CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL268175 11948 None 1 Human Binding pEC50 = 4.9 4.9 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 180 3 1 4 0.9 C=CCOc1noc2c1CNCC2 10.1021/jm00156a018
10465280 102840 None 0 Human Binding pEC50 = 6.9 6.9 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 196 2 1 4 1.5 CC(C)Oc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL305264 102840 None 0 Human Binding pEC50 = 6.9 6.9 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 196 2 1 4 1.5 CC(C)Oc1noc2c1CNCCC2 10.1021/jm00012a019
2166 3123 None 33 Human Binding pEC50 = 5.8 5.8 -6 7
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
305 3123 None 33 Human Binding pEC50 = 5.8 5.8 -6 7
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
5910 3123 None 33 Human Binding pEC50 = 5.8 5.8 -6 7
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
5910.0 3123 None 33 Human Binding pEC50 = 5.8 5.8 -6 7
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
CHEMBL550 3123 None 33 Human Binding pEC50 = 5.8 5.8 -6 7
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
DB01085 3123 None 33 Human Binding pEC50 = 5.8 5.8 -6 7
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1021/acs.jnatprod.2c01079
13621569 11957 None 1 Human Binding pEC50 = 5.8 5.8 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCOc1noc2c1CN(C)CC2 10.1021/jm00156a018
CHEMBL1182850 11957 None 1 Human Binding pEC50 = 5.8 5.8 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCOc1noc2c1CN(C)CC2 10.1021/jm00156a018
CHEMBL269706 11957 None 1 Human Binding pEC50 = 5.8 5.8 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCOc1noc2c1CN(C)CC2 10.1021/jm00156a018
171345098 194724 None 0 Human Binding pEC50 = 4.8 4.8 - 0
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5287096 194724 None 0 Human Binding pEC50 = 4.8 4.8 - 0
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5315302 194724 None 0 Human Binding pEC50 = 4.8 4.8 - 0
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
163282064 194368 None 0 Human Binding pEC50 = 4.8 4.8 - 0
Antagonist activity at M3 receptor (unknown origin)Antagonist activity at M3 receptor (unknown origin)
ChEMBL 380 2 0 3 4.0 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccc(F)cc1 10.1016/j.bmcl.2022.129048
CHEMBL5284728 194368 None 0 Human Binding pEC50 = 4.8 4.8 - 0
Antagonist activity at M3 receptor (unknown origin)Antagonist activity at M3 receptor (unknown origin)
ChEMBL 380 2 0 3 4.0 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccc(F)cc1 10.1016/j.bmcl.2022.129048
303 2978 None 15 Human Binding pEC50 = 5.8 5.8 -89 6
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
4629 2978 None 15 Human Binding pEC50 = 5.8 5.8 -89 6
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
8595 2978 None 15 Human Binding pEC50 = 5.8 5.8 -89 6
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
CHEMBL44674 2978 None 15 Human Binding pEC50 = 5.8 5.8 -89 6
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
125603 11070 None 3 Human Binding pEC50 = 5.8 5.8 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 154 1 1 4 0.3 COc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1177907 11070 None 3 Human Binding pEC50 = 5.8 5.8 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 154 1 1 4 0.3 COc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL6451 11070 None 3 Human Binding pEC50 = 5.8 5.8 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 154 1 1 4 0.3 COc1noc2c1CNCC2 10.1021/jm00156a018
2551 794 None 13 Human Binding pEC50 = 5.8 5.8 -346 11
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
2551.0 794 None 13 Human Binding pEC50 = 5.8 5.8 -346 11
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
298 794 None 13 Human Binding pEC50 = 5.8 5.8 -346 11
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
488 794 None 13 Human Binding pEC50 = 5.8 5.8 -346 11
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
CHEMBL965 794 None 13 Human Binding pEC50 = 5.8 5.8 -346 11
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
DB00411 794 None 13 Human Binding pEC50 = 5.8 5.8 -346 11
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
2551 794 None 13 Human Binding pEC50 = 5.7 5.7 -346 11
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
2551.0 794 None 13 Human Binding pEC50 = 5.7 5.7 -346 11
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
298 794 None 13 Human Binding pEC50 = 5.7 5.7 -346 11
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
488 794 None 13 Human Binding pEC50 = 5.7 5.7 -346 11
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
CHEMBL965 794 None 13 Human Binding pEC50 = 5.7 5.7 -346 11
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
DB00411 794 None 13 Human Binding pEC50 = 5.7 5.7 -346 11
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
156009673 178359 None 0 Human Binding pEC50 = 8.7 8.7 1 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4633816 178359 None 0 Human Binding pEC50 = 8.7 8.7 1 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650683 178359 None 0 Human Binding pEC50 = 8.7 8.7 1 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
156014812 178367 None 0 Human Binding pEC50 = 8.7 8.7 1 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4647437 178367 None 0 Human Binding pEC50 = 8.7 8.7 1 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650736 178367 None 0 Human Binding pEC50 = 8.7 8.7 1 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
13621572 11072 None 0 Human Binding pEC50 = 4.7 4.7 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCN1CCc2onc(OC)c2C1 10.1021/jm00156a018
CHEMBL1177910 11072 None 0 Human Binding pEC50 = 4.7 4.7 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCN1CCc2onc(OC)c2C1 10.1021/jm00156a018
CHEMBL6568 11072 None 0 Human Binding pEC50 = 4.7 4.7 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCN1CCc2onc(OC)c2C1 10.1021/jm00156a018
171347905 193848 None 0 Human Binding pEC50 = 4.7 4.7 - 0
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 166 2 1 3 0.5 O=C1C[C@@H](Cc2cnc[nH]2)CO1 10.1021/acs.jnatprod.2c01079
CHEMBL5272950 193848 None 0 Human Binding pEC50 = 4.7 4.7 - 0
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 166 2 1 3 0.5 O=C1C[C@@H](Cc2cnc[nH]2)CO1 10.1021/acs.jnatprod.2c01079
2551 794 None 13 Human Binding pEC50 = 7.7 7.7 -346 11
Agonist activity at human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as stimulation of beta-arrestin recruitment incubated 90 mins by PathHunter assayAgonist activity at human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as stimulation of beta-arrestin recruitment incubated 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.2c01376
2551.0 794 None 13 Human Binding pEC50 = 7.7 7.7 -346 11
Agonist activity at human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as stimulation of beta-arrestin recruitment incubated 90 mins by PathHunter assayAgonist activity at human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as stimulation of beta-arrestin recruitment incubated 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.2c01376
298 794 None 13 Human Binding pEC50 = 7.7 7.7 -346 11
Agonist activity at human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as stimulation of beta-arrestin recruitment incubated 90 mins by PathHunter assayAgonist activity at human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as stimulation of beta-arrestin recruitment incubated 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.2c01376
488 794 None 13 Human Binding pEC50 = 7.7 7.7 -346 11
Agonist activity at human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as stimulation of beta-arrestin recruitment incubated 90 mins by PathHunter assayAgonist activity at human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as stimulation of beta-arrestin recruitment incubated 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.2c01376
CHEMBL965 794 None 13 Human Binding pEC50 = 7.7 7.7 -346 11
Agonist activity at human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as stimulation of beta-arrestin recruitment incubated 90 mins by PathHunter assayAgonist activity at human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as stimulation of beta-arrestin recruitment incubated 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.2c01376
DB00411 794 None 13 Human Binding pEC50 = 7.7 7.7 -346 11
Agonist activity at human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as stimulation of beta-arrestin recruitment incubated 90 mins by PathHunter assayAgonist activity at human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as stimulation of beta-arrestin recruitment incubated 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.2c01376
302 2977 None 15 Human Binding pEC50 = 6.7 6.7 -309 7
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
4630 2977 None 15 Human Binding pEC50 = 6.7 6.7 -309 7
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
CHEMBL7634 2977 None 15 Human Binding pEC50 = 6.7 6.7 -309 7
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
2551 794 None 13 Human Binding pEC50 = 7.7 7.7 -346 11
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
2551.0 794 None 13 Human Binding pEC50 = 7.7 7.7 -346 11
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
298 794 None 13 Human Binding pEC50 = 7.7 7.7 -346 11
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
488 794 None 13 Human Binding pEC50 = 7.7 7.7 -346 11
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
CHEMBL965 794 None 13 Human Binding pEC50 = 7.7 7.7 -346 11
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
DB00411 794 None 13 Human Binding pEC50 = 7.7 7.7 -346 11
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
187 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
187.0 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
187 255 None 24 Human Binding pEC50 = 6.7 6.7 -26 9
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
187.0 255 None 24 Human Binding pEC50 = 6.7 6.7 -26 9
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
294 255 None 24 Human Binding pEC50 = 6.7 6.7 -26 9
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
65 255 None 24 Human Binding pEC50 = 6.7 6.7 -26 9
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
8593 255 None 24 Human Binding pEC50 = 6.7 6.7 -26 9
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
CHEMBL667 255 None 24 Human Binding pEC50 = 6.7 6.7 -26 9
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
DB03128 255 None 24 Human Binding pEC50 = 6.7 6.7 -26 9
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
187 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
187.0 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 255 None 24 Human Binding pEC50 = 7.6 7.6 -26 9
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
187 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
187.0 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
2551 794 None 13 Human Binding pEC50 = 7.6 7.6 -346 11
Agonist activity at human muscarinic M3 receptor expressed in human HEK293T cells assessed as activation of G-protein signaling by measuring inositol accumulation incubated for 90 mins by HTRF assayAgonist activity at human muscarinic M3 receptor expressed in human HEK293T cells assessed as activation of G-protein signaling by measuring inositol accumulation incubated for 90 mins by HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.2c01376
2551.0 794 None 13 Human Binding pEC50 = 7.6 7.6 -346 11
Agonist activity at human muscarinic M3 receptor expressed in human HEK293T cells assessed as activation of G-protein signaling by measuring inositol accumulation incubated for 90 mins by HTRF assayAgonist activity at human muscarinic M3 receptor expressed in human HEK293T cells assessed as activation of G-protein signaling by measuring inositol accumulation incubated for 90 mins by HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.2c01376
298 794 None 13 Human Binding pEC50 = 7.6 7.6 -346 11
Agonist activity at human muscarinic M3 receptor expressed in human HEK293T cells assessed as activation of G-protein signaling by measuring inositol accumulation incubated for 90 mins by HTRF assayAgonist activity at human muscarinic M3 receptor expressed in human HEK293T cells assessed as activation of G-protein signaling by measuring inositol accumulation incubated for 90 mins by HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.2c01376
488 794 None 13 Human Binding pEC50 = 7.6 7.6 -346 11
Agonist activity at human muscarinic M3 receptor expressed in human HEK293T cells assessed as activation of G-protein signaling by measuring inositol accumulation incubated for 90 mins by HTRF assayAgonist activity at human muscarinic M3 receptor expressed in human HEK293T cells assessed as activation of G-protein signaling by measuring inositol accumulation incubated for 90 mins by HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.2c01376
CHEMBL965 794 None 13 Human Binding pEC50 = 7.6 7.6 -346 11
Agonist activity at human muscarinic M3 receptor expressed in human HEK293T cells assessed as activation of G-protein signaling by measuring inositol accumulation incubated for 90 mins by HTRF assayAgonist activity at human muscarinic M3 receptor expressed in human HEK293T cells assessed as activation of G-protein signaling by measuring inositol accumulation incubated for 90 mins by HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.2c01376
DB00411 794 None 13 Human Binding pEC50 = 7.6 7.6 -346 11
Agonist activity at human muscarinic M3 receptor expressed in human HEK293T cells assessed as activation of G-protein signaling by measuring inositol accumulation incubated for 90 mins by HTRF assayAgonist activity at human muscarinic M3 receptor expressed in human HEK293T cells assessed as activation of G-protein signaling by measuring inositol accumulation incubated for 90 mins by HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.2c01376
154059 3637 None 37 Human Binding pEC50 = 7.6 7.6 -1 8
Antagonist activity at M3 receptor (unknown origin)Antagonist activity at M3 receptor (unknown origin)
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2022.129048
154059.0 3637 None 37 Human Binding pEC50 = 7.6 7.6 -1 8
Antagonist activity at M3 receptor (unknown origin)Antagonist activity at M3 receptor (unknown origin)
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2022.129048
2457 3637 None 37 Human Binding pEC50 = 7.6 7.6 -1 8
Antagonist activity at M3 receptor (unknown origin)Antagonist activity at M3 receptor (unknown origin)
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2022.129048
7483 3637 None 37 Human Binding pEC50 = 7.6 7.6 -1 8
Antagonist activity at M3 receptor (unknown origin)Antagonist activity at M3 receptor (unknown origin)
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2022.129048
CHEMBL1734 3637 None 37 Human Binding pEC50 = 7.6 7.6 -1 8
Antagonist activity at M3 receptor (unknown origin)Antagonist activity at M3 receptor (unknown origin)
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2022.129048
DB01591 3637 None 37 Human Binding pEC50 = 7.6 7.6 -1 8
Antagonist activity at M3 receptor (unknown origin)Antagonist activity at M3 receptor (unknown origin)
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2022.129048
187 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
187.0 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 255 None 24 Human Binding pEC50 = 6.6 6.6 -26 9
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
156015097 177657 None 0 Human Binding pEC50 = 7.6 7.6 1 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4640324 177657 None 0 Human Binding pEC50 = 7.6 7.6 1 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
156015300 177697 None 0 Human Binding pEC50 = 7.6 7.6 4 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640703 177697 None 0 Human Binding pEC50 = 7.6 7.6 4 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
156021744 178219 None 0 Human Binding pEC50 = 7.6 7.6 1 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4648071 178219 None 0 Human Binding pEC50 = 7.6 7.6 1 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
171348452 194741 None 0 Human Binding pEC50 = 5.6 5.6 - 0
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5285668 194741 None 0 Human Binding pEC50 = 5.6 5.6 - 0
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5315497 194741 None 0 Human Binding pEC50 = 5.6 5.6 - 0
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 602 14 0 5 5.2 CC[C@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
160492 97310 None 26 Human Binding pEC50 = 6.5 6.5 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 141 1 1 3 0.1 COC(=O)C1=CCCNC1 10.1021/jm00156a018
CHEMBL268808 97310 None 26 Human Binding pEC50 = 6.5 6.5 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 141 1 1 3 0.1 COC(=O)C1=CCCNC1 10.1021/jm00156a018
171346325 194774 None 0 Human Binding pEC50 = 4.5 4.5 - 0
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 630 16 0 5 5.9 CC[C@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5277944 194774 None 0 Human Binding pEC50 = 4.5 4.5 - 0
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 630 16 0 5 5.9 CC[C@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
CHEMBL5316061 194774 None 0 Human Binding pEC50 = 4.5 4.5 - 0
Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayPartial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 630 16 0 5 5.9 CC[C@H]1C(=O)OC[C@@H]1Cc1c[n+](CCCCCCCC[N+](C)(C)CC(C)(C)CN2C(=O)c3cccc4cccc(c34)C2=O)cn1C 10.1021/acs.jnatprod.2c01079
2230 465 None 43 Human Binding pEC50 = 6.5 6.5 -588 10
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
296 465 None 43 Human Binding pEC50 = 6.5 6.5 -588 10
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
CHEMBL7303 465 None 43 Human Binding pEC50 = 6.5 6.5 -588 10
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
DB04365 465 None 43 Human Binding pEC50 = 6.5 6.5 -588 10
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
13621545 11073 None 3 Human Binding pEC50 = 5.5 5.5 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 2 1 4 0.7 CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1177913 11073 None 3 Human Binding pEC50 = 5.5 5.5 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 2 1 4 0.7 CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL6680 11073 None 3 Human Binding pEC50 = 5.5 5.5 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 2 1 4 0.7 CCOc1noc2c1CNCC2 10.1021/jm00156a018
137629935 161114 None 0 Human Binding pEC50 = 5.4 5.4 -1 3
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4060823 161114 None 0 Human Binding pEC50 = 5.4 5.4 -1 3
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116342 161114 None 0 Human Binding pEC50 = 5.4 5.4 -1 3
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
156011965 177397 None 0 Human Binding pEC50 = 8.4 8.4 3 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636528 177397 None 0 Human Binding pEC50 = 8.4 8.4 3 3
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
13621565 11079 None 1 Human Binding pEC50 = 5.4 5.4 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 192 2 1 4 0.7 CC#CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1177927 11079 None 1 Human Binding pEC50 = 5.4 5.4 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 192 2 1 4 0.7 CC#CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL7018 11079 None 1 Human Binding pEC50 = 5.4 5.4 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 192 2 1 4 0.7 CC#CCOc1noc2c1CNCC2 10.1021/jm00156a018
10442337 206406 None 1 Human Binding pEC50 = 6.3 6.3 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 182 2 1 4 1.1 CCOc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL69305 206406 None 1 Human Binding pEC50 = 6.3 6.3 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 182 2 1 4 1.1 CCOc1noc2c1CNCCC2 10.1021/jm00012a019
187 255 None 24 Human Binding pEC50 = 6.3 6.3 -26 9
Agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
187.0 255 None 24 Human Binding pEC50 = 6.3 6.3 -26 9
Agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
294 255 None 24 Human Binding pEC50 = 6.3 6.3 -26 9
Agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
65 255 None 24 Human Binding pEC50 = 6.3 6.3 -26 9
Agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
8593 255 None 24 Human Binding pEC50 = 6.3 6.3 -26 9
Agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
CHEMBL667 255 None 24 Human Binding pEC50 = 6.3 6.3 -26 9
Agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
DB03128 255 None 24 Human Binding pEC50 = 6.3 6.3 -26 9
Agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assayAgonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jnatprod.2c01079
10442081 102663 None 6 Human Binding pEC50 = 6.2 6.2 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 168 1 1 4 0.7 COc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL304142 102663 None 6 Human Binding pEC50 = 6.2 6.2 - 0
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 168 1 1 4 0.7 COc1noc2c1CNCCC2 10.1021/jm00012a019
3008304 4023 None 46 Human Binding pEC50 = 5.2 5.2 - 0
Positive allosteric modulation activity at muscarinic M3 receptorPositive allosteric modulation activity at muscarinic M3 receptor
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm201139r
7632 4023 None 46 Human Binding pEC50 = 5.2 5.2 - 0
Positive allosteric modulation activity at muscarinic M3 receptorPositive allosteric modulation activity at muscarinic M3 receptor
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm201139r
CHEMBL523685 4023 None 46 Human Binding pEC50 = 5.2 5.2 - 0
Positive allosteric modulation activity at muscarinic M3 receptorPositive allosteric modulation activity at muscarinic M3 receptor
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm201139r
2551 794 None 13 Human Binding pEC50 = 7.2 7.2 -346 11
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
2551.0 794 None 13 Human Binding pEC50 = 7.2 7.2 -346 11
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
298 794 None 13 Human Binding pEC50 = 7.2 7.2 -346 11
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
488 794 None 13 Human Binding pEC50 = 7.2 7.2 -346 11
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
CHEMBL965 794 None 13 Human Binding pEC50 = 7.2 7.2 -346 11
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
DB00411 794 None 13 Human Binding pEC50 = 7.2 7.2 -346 11
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
13621567 98213 None 4 Human Binding pEC50 = 6.1 6.1 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 1 0 4 0.7 COc1noc2c1CN(C)CC2 10.1021/jm00156a018
CHEMBL27384 98213 None 4 Human Binding pEC50 = 6.1 6.1 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 1 0 4 0.7 COc1noc2c1CN(C)CC2 10.1021/jm00156a018
CHEMBL440085 98213 None 4 Human Binding pEC50 = 6.1 6.1 - 0
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 1 0 4 0.7 COc1noc2c1CN(C)CC2 10.1021/jm00156a018
57400422 71655 None 0 Human Binding pIC50 = 10.5 10.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 330 4 0 2 3.9 C[C@@](C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924027 71655 None 0 Human Binding pIC50 = 10.5 10.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 330 4 0 2 3.9 C[C@@](C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1963462 71655 None 0 Human Binding pIC50 = 10.5 10.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 330 4 0 2 3.9 C[C@@](C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
24758141 103782 None 0 Human Binding pIC50 = 10.5 10.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 4 0 2 3.9 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087959 103782 None 0 Human Binding pIC50 = 10.5 10.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 4 0 2 3.9 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2013.09.092
367 3824 None 10 Human Binding pIC50 = 10.3 10.3 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
5487427 3824 None 10 Human Binding pIC50 = 10.3 10.3 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
5487427.0 3824 None 10 Human Binding pIC50 = 10.3 10.3 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
8592 3824 None 10 Human Binding pIC50 = 10.3 10.3 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
CHEMBL1900528 3824 None 10 Human Binding pIC50 = 10.3 10.3 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
CHEMBL3305968 3824 None 10 Human Binding pIC50 = 10.3 10.3 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
CHEMBL4650755 3824 None 10 Human Binding pIC50 = 10.3 10.3 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
DB01409 3824 None 10 Human Binding pIC50 = 10.3 10.3 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
57392578 68769 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 487 7 0 4 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc(Cl)s3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921908 68769 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 487 7 0 4 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc(Cl)s3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395222 69170 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 5.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924040 69170 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 5.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545528 103690 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 453 7 0 4 5.5 O=C(O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)C1(c2cccs2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087230 103690 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 453 7 0 4 5.5 O=C(O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)C1(c2cccs2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545784 103694 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 475 7 0 4 6.1 O=C(O[C@H]1C[N+]2(CCCc3nc4ccccc4o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087235 103694 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 475 7 0 4 6.1 O=C(O[C@H]1C[N+]2(CCCc3nc4ccccc4o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
57401273 68768 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 525 7 0 3 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cccc(Br)c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921907 68768 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 525 7 0 3 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cccc(Br)c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57394170 68783 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 517 8 0 4 6.4 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cc4ccccc4s3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921925 68783 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 517 8 0 4 6.4 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cc4ccccc4s3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57394234 68793 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 483 9 0 5 5.1 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921935 68793 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 483 9 0 5 5.1 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
59179619 103784 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 327 3 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)C1(c2ccccc2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087961 103784 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 327 3 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)C1(c2ccccc2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545282 103791 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 440 6 0 3 6.0 Cc1ccc(CC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)s1 10.1016/j.bmcl.2013.09.092
CHEMBL3088081 103791 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 440 6 0 3 6.0 Cc1ccc(CC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)s1 10.1016/j.bmcl.2013.09.092
72545526 103795 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 8 0 3 5.8 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088086 103795 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 8 0 3 5.8 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
57390665 68775 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 462 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921917 68775 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 462 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395990 68795 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 501 9 0 5 5.2 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921937 68795 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 501 9 0 5 5.2 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546493 103780 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 473 6 0 4 6.2 O=C(O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)on3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087957 103780 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 473 6 0 4 6.2 O=C(O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)on3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
58348375 103785 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 333 3 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)C1(c2cccs2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088075 103785 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 333 3 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)C1(c2cccs2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545281 103790 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 420 6 0 2 5.6 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088080 103790 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 420 6 0 2 5.6 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
57395991 68803 None 0 Human Binding pIC50 = 10 10.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 500 7 1 5 4.4 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccc(F)c3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921945 68803 None 0 Human Binding pIC50 = 10 10.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 500 7 1 5 4.4 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccc(F)c3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57391636 68858 None 0 Human Binding pIC50 = 10 10.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 518 7 1 7 3.7 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cncc(Cl)n3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922053 68858 None 0 Human Binding pIC50 = 10 10.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 518 7 1 7 3.7 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cncc(Cl)n3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988645 69166 None 0 Human Binding pIC50 = 10 10.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 351 4 0 4 3.2 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924036 69166 None 0 Human Binding pIC50 = 10 10.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 351 4 0 4 3.2 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546026 103700 None 0 Human Binding pIC50 = 10 10.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 439 6 2 4 3.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cc[nH]n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087242 103700 None 0 Human Binding pIC50 = 10 10.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 439 6 2 4 3.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cc[nH]n1 10.1016/j.bmcl.2013.09.092
72543916 103772 None 0 Human Binding pIC50 = 10 10.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 485 6 1 5 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cncc(Cl)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087949 103772 None 0 Human Binding pIC50 = 10 10.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 485 6 1 5 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cncc(Cl)n1 10.1016/j.bmcl.2013.09.092
72546261 103775 None 0 Human Binding pIC50 = 10 10.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 447 5 0 4 5.7 O=C(O[C@H]1C[N+]2(Cc3nc4ccccc4o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087952 103775 None 0 Human Binding pIC50 = 10 10.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 447 5 0 4 5.7 O=C(O[C@H]1C[N+]2(Cc3nc4ccccc4o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
11434515 261 None 6 Human Binding pIC50 = 9.9 9.9 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
11434515.0 261 None 6 Human Binding pIC50 = 9.9 9.9 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
11519741 261 None 6 Human Binding pIC50 = 9.9 9.9 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
4484 261 None 6 Human Binding pIC50 = 9.9 9.9 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
7449 261 None 6 Human Binding pIC50 = 9.9 9.9 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
CHEMBL1194325 261 None 6 Human Binding pIC50 = 9.9 9.9 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
DB08897 261 None 6 Human Binding pIC50 = 9.9 9.9 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
44552684 68777 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 8 0 4 4.9 Cc1cc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)ccn1 10.1016/j.bmcl.2011.10.002
CHEMBL1921919 68777 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 8 0 4 4.9 Cc1cc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)ccn1 10.1016/j.bmcl.2011.10.002
57397792 68799 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 406 6 1 5 2.1 C[C@@](C(=O)O[C@H]1C[N+]2(CC(N)=O)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921941 68799 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 406 6 1 5 2.1 C[C@@](C(=O)O[C@H]1C[N+]2(CC(N)=O)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57401219 68804 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 7 1 5 3.6 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921946 68804 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 7 1 5 3.6 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57391775 69177 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 465 7 0 3 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccccc3F)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924049 69177 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 465 7 0 3 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccccc3F)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
11693 1827 None 12 Human Binding pIC50 = 9.9 9.9 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
3494 1827 None 12 Human Binding pIC50 = 9.9 9.9 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
3494.0 1827 None 12 Human Binding pIC50 = 9.9 9.9 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
4302 1827 None 12 Human Binding pIC50 = 9.9 9.9 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
7459 1827 None 12 Human Binding pIC50 = 9.9 9.9 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
9933193 1827 None 12 Human Binding pIC50 = 9.9 9.9 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
9933193.0 1827 None 12 Human Binding pIC50 = 9.9 9.9 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
CHEMBL1201335 1827 None 12 Human Binding pIC50 = 9.9 9.9 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
DB00986 1827 None 12 Human Binding pIC50 = 9.9 9.9 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
72545787 103697 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 467 6 1 3 5.1 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccc(F)c1 10.1016/j.bmcl.2013.09.092
CHEMBL3087238 103697 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 467 6 1 3 5.1 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccc(F)c1 10.1016/j.bmcl.2013.09.092
72545525 103794 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 8 0 3 5.6 O=C(O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088085 103794 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 8 0 3 5.6 O=C(O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
44517831 68767 None 4 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 465 7 0 3 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921904 68767 None 4 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 465 7 0 3 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395952 68771 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 491 7 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCC3=CC4CCOC4C=C3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921911 68771 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 491 7 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCC3=CC4CCOC4C=C3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397744 68776 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 468 8 0 5 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921918 68776 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 468 8 0 5 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57390720 68856 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 467 7 1 6 3.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccon3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922051 68856 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 467 7 1 6 3.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccon3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57403853 68859 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 488 6 0 5 5.2 Cc1ccc2nc(C[N+]34CCC(CC3)[C@@H](OC(=O)[C@](C)(c3ccccc3)N3CCCCC3)C4)oc2c1 10.1016/j.bmcl.2011.10.002
CHEMBL1922054 68859 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 488 6 0 5 5.2 Cc1ccc2nc(C[N+]34CCC(CC3)[C@@H](OC(=O)[C@](C)(c3ccccc3)N3CCCCC3)C4)oc2c1 10.1016/j.bmcl.2011.10.002
57398751 69157 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 471 7 0 4 5.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccccc3F)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924025 69157 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 471 7 0 4 5.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccccc3F)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545530 103691 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 449 7 0 3 5.7 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087232 103691 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 449 7 0 3 5.7 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
72546025 103699 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 454 6 1 5 4.3 Cc1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)no1 10.1016/j.bmcl.2013.09.092
CHEMBL3087241 103699 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 454 6 1 5 4.3 Cc1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)no1 10.1016/j.bmcl.2013.09.092
72546496 103713 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087362 103713 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccn1 10.1016/j.bmcl.2013.09.092
72546739 103718 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccncn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087367 103718 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccncn1 10.1016/j.bmcl.2013.09.092
72546991 103719 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccnn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087368 103719 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccnn1 10.1016/j.bmcl.2013.09.092
72546262 103776 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 474 6 0 5 5.6 O=C(O[C@H]1C[N+]2(Cc3nc(-c4ccccc4)no3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087953 103776 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 474 6 0 5 5.6 O=C(O[C@H]1C[N+]2(Cc3nc(-c4ccccc4)no3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545285 103793 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 436 7 0 3 5.4 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088084 103793 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 436 7 0 3 5.4 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
11434515 261 None 6 Human Binding pIC50 = 9.8 9.8 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
11434515.0 261 None 6 Human Binding pIC50 = 9.8 9.8 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
11519741 261 None 6 Human Binding pIC50 = 9.8 9.8 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
4484 261 None 6 Human Binding pIC50 = 9.8 9.8 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
7449 261 None 6 Human Binding pIC50 = 9.8 9.8 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
CHEMBL1194325 261 None 6 Human Binding pIC50 = 9.8 9.8 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
DB08897 261 None 6 Human Binding pIC50 = 9.8 9.8 -4 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
10143956 13916 None 0 Human Binding pIC50 = 9.7 9.7 -1 3
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL1196359 13916 None 0 Human Binding pIC50 = 9.7 9.7 -1 3
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL556635 13916 None 0 Human Binding pIC50 = 9.7 9.7 -1 3
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
57390766 68770 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 497 7 0 3 5.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc4ccccc4c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921910 68770 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 497 7 0 3 5.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc4ccccc4c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57402931 68774 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 459 7 0 4 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCC3CCCCC3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921914 68774 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 459 7 0 4 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCC3CCCCC3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57399407 68785 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 475 9 0 3 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921927 68785 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 475 9 0 3 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57401217 68798 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 400 6 1 4 2.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(N)=O)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921940 68798 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 400 6 1 4 2.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(N)=O)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397793 68800 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 7 1 4 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921942 68800 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 7 1 4 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57401218 68801 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 482 7 1 5 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921943 68801 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 482 7 1 5 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397794 68802 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 494 7 1 4 4.3 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccc(F)c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921944 68802 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 494 7 1 4 4.3 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccc(F)c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57392520 68855 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cnccn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922050 68855 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cnccn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57392521 68857 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 473 7 1 7 3.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccon3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922052 68857 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 473 7 1 7 3.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccon3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395096 68860 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 500 7 0 5 5.4 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)on3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922055 68860 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 500 7 0 5 5.4 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)on3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545785 103695 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 373 5 1 3 2.9 NC(=O)C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2 10.1016/j.bmcl.2013.09.092
CHEMBL3087236 103695 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 373 5 1 3 2.9 NC(=O)C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2 10.1016/j.bmcl.2013.09.092
72546736 103715 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccnc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087364 103715 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccnc1 10.1016/j.bmcl.2013.09.092
72547500 103769 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 485 6 1 5 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(Cl)nn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087946 103769 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 485 6 1 5 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(Cl)nn1 10.1016/j.bmcl.2013.09.092
10165877 63150 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779133 63150 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789396 63150 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
11852298 14031 None 0 Human Binding pIC50 = 9.7 9.7 -1 3
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1197251 14031 None 0 Human Binding pIC50 = 9.7 9.7 -1 3
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL564057 14031 None 0 Human Binding pIC50 = 9.7 9.7 -1 3
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
71524764 144528 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 833 16 5 14 6.5 COc1cc(-c2noc(CCCN(C)[C@H]3CC[C@H](OC(=O)C(O)(c4cccs4)c4cccs4)CC3)n2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3906438 144528 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 833 16 5 14 6.5 COc1cc(-c2noc(CCCN(C)[C@H]3CC[C@H](OC(=O)C(O)(c4cccs4)c4cccs4)CC3)n2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
54592025 148083 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 695 18 5 10 6.4 CN(CCCCCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3934254 148083 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 695 18 5 10 6.4 CN(CCCCCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
44232927 197793 None 8 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 349 4 1 6 2.7 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL551729 197793 None 8 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 349 4 1 6 2.7 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
86765983 145902 None 0 Human Binding pIC50 = 9.6 9.6 - 1
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 342 4 0 2 4.1 C[C@@](C(=O)O[C@@H]1CC2CCC1[N+]2(C)C)(c1ccccc1)C1CCCC1 nan
CHEMBL3917058 145902 None 0 Human Binding pIC50 = 9.6 9.6 - 1
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 342 4 0 2 4.1 C[C@@](C(=O)O[C@@H]1CC2CCC1[N+]2(C)C)(c1ccccc1)C1CCCC1 nan
44233401 13629 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 10.1021/jm900132z
CHEMBL1194321 13629 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 10.1021/jm900132z
CHEMBL551327 13629 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 10.1021/jm900132z
44233177 13905 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL1196246 13905 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL556221 13905 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 10.1021/jm900132z
44233403 13906 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL1196247 13906 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL556222 13906 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
53372934 129368 None 0 Human Binding pIC50 = 9.6 9.6 - 1
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670826 129368 None 0 Human Binding pIC50 = 9.6 9.6 - 1
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
53372936 129369 None 0 Human Binding pIC50 = 9.6 9.6 - 1
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670827 129369 None 0 Human Binding pIC50 = 9.6 9.6 - 1
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
11693 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
3494 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
3494.0 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
4302 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
7459 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
9933193 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
9933193.0 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
CHEMBL1201335 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
DB00986 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
11693 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
3494 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
3494.0 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
4302 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
7459 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
9933193 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
9933193.0 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
CHEMBL1201335 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
DB00986 1827 None 12 Human Binding pIC50 = 9.6 9.6 -1 5
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
57392462 68786 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 481 9 0 4 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921928 68786 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 481 9 0 4 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57400294 68863 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 507 7 0 7 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3noc(-c4ccccc4)n3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922058 68863 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 507 7 0 7 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3noc(-c4ccccc4)n3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988644 69159 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 345 4 0 3 3.2 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924029 69159 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 345 4 0 3 3.2 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545786 103696 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 449 6 1 3 5.0 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087237 103696 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 449 6 1 3 5.0 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccc1 10.1016/j.bmcl.2013.09.092
72546993 103720 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 468 6 1 4 4.5 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncccc1F 10.1016/j.bmcl.2013.09.092
CHEMBL3087370 103720 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 468 6 1 4 4.5 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncccc1F 10.1016/j.bmcl.2013.09.092
72547254 103725 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 518 6 1 4 5.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(C(F)(F)F)nc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087375 103725 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 518 6 1 4 5.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(C(F)(F)F)nc1 10.1016/j.bmcl.2013.09.092
72546263 103777 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 473 6 0 4 6.2 O=C(O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)no3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087954 103777 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 473 6 0 4 6.2 O=C(O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)no3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
69167248 103783 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 3 0 2 4.1 C[N+]1(C)CCC(OC(=O)C2(c3ccccc3)CCCCCC2)CC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087960 103783 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 3 0 2 4.1 C[N+]1(C)CCC(OC(=O)C2(c3ccccc3)CCCCCC2)CC1 10.1016/j.bmcl.2013.09.092
44236101 14033 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL1197261 14033 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL564515 14033 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
10208897 63147 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 455 8 0 2 6.1 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779049 63147 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 455 8 0 2 6.1 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789387 63147 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 455 8 0 2 6.1 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
10143718 63154 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779131 63154 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789435 63154 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
71558563 143867 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 758 14 5 13 5.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3900995 143867 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 758 14 5 13 5.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
54673357 145701 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 795 17 5 12 6.7 COc1cc(OCCCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3915601 145701 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 795 17 5 12 6.7 COc1cc(OCCCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
53372938 129370 None 0 Human Binding pIC50 = 9.5 9.5 - 1
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670828 129370 None 0 Human Binding pIC50 = 9.5 9.5 - 1
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
1734 116 None 5 Human Binding pIC50 = 9.5 9.5 1 12
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
307 116 None 5 Human Binding pIC50 = 9.5 9.5 1 12
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
CHEMBL168067 116 None 5 Human Binding pIC50 = 9.5 9.5 1 12
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
11569908 14006 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL1197028 14006 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL559106 14006 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
44232930 199149 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 343 4 1 5 2.6 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL564747 199149 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 343 4 1 5 2.6 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
57399406 68779 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 462 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cccnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921921 68779 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 462 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cccnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397746 68782 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 502 8 0 5 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3nc4ccccc4o3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921924 68782 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 502 8 0 5 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3nc4ccccc4o3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57394233 68790 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 8 0 4 4.9 Cc1ccc(OCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cc1 10.1016/j.bmcl.2011.10.002
CHEMBL1921932 68790 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 8 0 4 4.9 Cc1ccc(OCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cc1 10.1016/j.bmcl.2011.10.002
57395097 68861 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 501 7 0 6 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3nc(-c4ccccc4)no3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922056 68861 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 501 7 0 6 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3nc(-c4ccccc4)no3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546494 103781 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 474 6 0 5 5.6 O=C(O[C@H]1C[N+]2(Cc3nnc(-c4ccccc4)o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087958 103781 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 474 6 0 5 5.6 O=C(O[C@H]1C[N+]2(Cc3nnc(-c4ccccc4)o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
367 3824 None 10 Human Binding pIC50 = 9.5 9.5 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
5487427 3824 None 10 Human Binding pIC50 = 9.5 9.5 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
5487427.0 3824 None 10 Human Binding pIC50 = 9.5 9.5 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
8592 3824 None 10 Human Binding pIC50 = 9.5 9.5 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL1900528 3824 None 10 Human Binding pIC50 = 9.5 9.5 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL3305968 3824 None 10 Human Binding pIC50 = 9.5 9.5 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL4650755 3824 None 10 Human Binding pIC50 = 9.5 9.5 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
DB01409 3824 None 10 Human Binding pIC50 = 9.5 9.5 2 9
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
20735153 13628 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1194314 13628 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL551063 13628 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1021/jm900132z
11489419 13623 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 448 10 1 5 5.2 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
CHEMBL1194274 13623 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 448 10 1 5 5.2 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
CHEMBL549784 13623 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 448 10 1 5 5.2 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
44232931 198837 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 4 1 5 2.8 O=C(O[C@H]1CN2CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL562642 198837 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 4 1 5 2.8 O=C(O[C@H]1CN2CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
57390666 68784 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 518 8 0 5 5.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccc4ncsc4c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921926 68784 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 518 8 0 5 5.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccc4ncsc4c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57396866 68862 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 506 7 0 6 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)no3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922057 68862 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 506 7 0 6 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)no3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546028 103702 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 457 6 1 6 3.9 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncns1 10.1016/j.bmcl.2013.09.092
CHEMBL3087244 103702 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 457 6 1 6 3.9 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncns1 10.1016/j.bmcl.2013.09.092
72547256 103727 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1nccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087377 103727 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1nccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
72546264 103778 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 472 6 0 4 5.8 O=C(O[C@H]1C[N+]2(Cc3ccn(-c4ccccc4)n3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087955 103778 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 472 6 0 4 5.8 O=C(O[C@H]1C[N+]2(Cc3ccn(-c4ccccc4)n3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
367 3824 None 10 Human Binding pIC50 = 9.4 9.4 2 9
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
5487427 3824 None 10 Human Binding pIC50 = 9.4 9.4 2 9
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
5487427.0 3824 None 10 Human Binding pIC50 = 9.4 9.4 2 9
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
8592 3824 None 10 Human Binding pIC50 = 9.4 9.4 2 9
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
CHEMBL1900528 3824 None 10 Human Binding pIC50 = 9.4 9.4 2 9
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
CHEMBL3305968 3824 None 10 Human Binding pIC50 = 9.4 9.4 2 9
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
CHEMBL4650755 3824 None 10 Human Binding pIC50 = 9.4 9.4 2 9
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
DB01409 3824 None 10 Human Binding pIC50 = 9.4 9.4 2 9
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
71556977 142631 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 769 15 5 13 5.9 CN(CCCc1nc(-c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)no1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3890898 142631 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 769 15 5 13 5.9 CN(CCCc1nc(-c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)no1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
71566009 144395 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 838 17 5 13 5.4 COc1cc(OCC(=O)N(C)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3905320 144395 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 838 17 5 13 5.4 COc1cc(OCC(=O)N(C)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
71558416 151416 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 757 14 6 12 4.9 CN(CCCn1c(=O)[nH]c2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3961014 151416 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 757 14 6 12 4.9 CN(CCCn1c(=O)[nH]c2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
121347973 151717 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 732 14 5 13 4.6 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4c3OCC(=O)N4)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
CHEMBL3963770 151717 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 732 14 5 13 4.6 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4c3OCC(=O)N4)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
1734 116 None 5 Human Binding pIC50 = 9.4 9.4 1 12
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
307 116 None 5 Human Binding pIC50 = 9.4 9.4 1 12
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
CHEMBL168067 116 None 5 Human Binding pIC50 = 9.4 9.4 1 12
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
1734 116 None 5 Human Binding pIC50 = 9.4 9.4 1 12
Displacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
307 116 None 5 Human Binding pIC50 = 9.4 9.4 1 12
Displacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
CHEMBL168067 116 None 5 Human Binding pIC50 = 9.4 9.4 1 12
Displacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
44236098 198104 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 343 4 1 5 2.6 O=C(O[C@H]1CN2CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL556426 198104 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 343 4 1 5 2.6 O=C(O[C@H]1CN2CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
1734 116 None 5 Human Binding pIC50 = 9.4 9.4 1 12
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
307 116 None 5 Human Binding pIC50 = 9.4 9.4 1 12
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
CHEMBL168067 116 None 5 Human Binding pIC50 = 9.4 9.4 1 12
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
44236340 13797 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1195513 13797 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL554725 13797 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
44232685 14034 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL1197273 14034 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL564765 14034 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
10119939 63148 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1777827 63148 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789388 63148 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
71558718 144810 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 14 5 13 5.7 CN(CCCn1c(=O)sc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3908788 144810 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 14 5 13 5.7 CN(CCCn1c(=O)sc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
57392515 68797 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 491 10 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOCCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921939 68797 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 491 10 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOCCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545783 103693 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 438 7 0 4 4.7 Cn1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087234 103693 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 438 7 0 4 4.7 Cn1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
72546994 103721 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)nc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087371 103721 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)nc1 10.1016/j.bmcl.2013.09.092
1734 116 None 5 Human Binding pIC50 = 9.3 9.3 1 12
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
307 116 None 5 Human Binding pIC50 = 9.3 9.3 1 12
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
CHEMBL168067 116 None 5 Human Binding pIC50 = 9.3 9.3 1 12
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
44232681 14020 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 0 5 5.7 CC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1197156 14020 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 0 5 5.7 CC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL561187 14020 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 0 5 5.7 CC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)c1cccs1 10.1021/jm900132z
1734 116 None 5 Human Binding pIC50 = 9.2 9.2 1 12
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
307 116 None 5 Human Binding pIC50 = 9.2 9.2 1 12
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
CHEMBL168067 116 None 5 Human Binding pIC50 = 9.2 9.2 1 12
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
9928017 62359 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 342 4 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779033 62359 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 342 4 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
10229167 63145 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 427 9 0 3 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779136 63145 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 427 9 0 3 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789385 63145 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 427 9 0 3 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
10393952 63149 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 529 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779140 63149 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 529 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1789389 63149 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 529 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
10187216 63158 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 461 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779128 63158 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 461 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789452 63158 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 461 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
10143858 63159 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779132 63159 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789454 63159 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
44236336 14018 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 364 4 1 5 2.8 C[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
CHEMBL1197131 14018 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 364 4 1 5 2.8 C[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
CHEMBL560327 14018 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 364 4 1 5 2.8 C[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
71558567 142768 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 740 14 5 11 6.2 CN(CCCn1ccc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3892021 142768 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 740 14 5 11 6.2 CN(CCCn1ccc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
121347950 151321 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 728 14 5 12 5.1 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
CHEMBL3960091 151321 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 728 14 5 12 5.1 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
44232683 13631 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
CHEMBL1194336 13631 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
CHEMBL551731 13631 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
57399408 68787 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 463 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921929 68787 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 463 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395989 68794 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 495 9 0 4 5.1 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921936 68794 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 495 9 0 4 5.1 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57391773 69176 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 425 7 0 3 4.9 CC(C)=CCC[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
CHEMBL1924046 69176 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 425 7 0 3 4.9 CC(C)=CCC[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
72546738 103717 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cncnc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087366 103717 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cncnc1 10.1016/j.bmcl.2013.09.092
72546995 103722 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 468 6 1 4 4.5 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(F)cn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087372 103722 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 468 6 1 4 4.5 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(F)cn1 10.1016/j.bmcl.2013.09.092
72543915 103771 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cncc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087948 103771 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cncc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
10007638 120940 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 8 2 4 4.4 O=C(N[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401648 120940 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 8 2 4 4.4 O=C(N[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559195 120940 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 8 2 4 4.4 O=C(N[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
67548926 120942 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 473 8 2 5 4.5 O=C(N[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401649 120942 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 473 8 2 5 4.5 O=C(N[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559201 120942 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 473 8 2 5 4.5 O=C(N[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
10325942 120943 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 8 2 5 3.9 O=C(N[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401650 120943 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 8 2 5 3.9 O=C(N[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559202 120943 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 8 2 5 3.9 O=C(N[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
44236099 198011 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 4 1 5 2.8 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL554699 198011 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 4 1 5 2.8 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
54673354 148814 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 808 16 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3940214 148814 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 808 16 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
44236332 14022 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL1197183 14022 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL561870 14022 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
72548703 161661 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]4-DAMP from human recombinant M3 receptor after 60 mins by scintillation counting analysisDisplacement of [3H]4-DAMP from human recombinant M3 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161661 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]4-DAMP from human recombinant M3 receptor after 60 mins by scintillation counting analysisDisplacement of [3H]4-DAMP from human recombinant M3 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
939077 197315 None 0 Human Binding pIC50 = 9.1 9.1 - 1
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 2 0 4 3.6 O=C(O[C@H]1CN2CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL549577 197315 None 0 Human Binding pIC50 = 9.1 9.1 - 1
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 2 0 4 3.6 O=C(O[C@H]1CN2CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
57397791 68796 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921938 68796 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57402222 69160 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 353 4 0 3 3.6 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1C=CC=CC=C1 10.1016/j.bmcl.2011.10.002
CHEMBL1924030 69160 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 353 4 0 3 3.6 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1C=CC=CC=C1 10.1016/j.bmcl.2011.10.002
57397002 69161 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 363 4 0 4 2.7 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCSCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924031 69161 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 363 4 0 4 2.7 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCSCC1 10.1016/j.bmcl.2011.10.002
72547252 103723 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccnc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c1 10.1016/j.bmcl.2013.09.092
CHEMBL3087373 103723 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccnc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c1 10.1016/j.bmcl.2013.09.092
72547255 103726 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087376 103726 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
72547498 103729 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)nn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087379 103729 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)nn1 10.1016/j.bmcl.2013.09.092
72547501 103770 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cnc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087947 103770 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cnc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
11678378 120950 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 7 1 3 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2015.02.065
CHEMBL3401654 120950 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 7 1 3 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2015.02.065
CHEMBL3559211 120950 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 7 1 3 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2015.02.065
10164137 63146 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 423 9 0 3 5.1 CCCCN(C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779137 63146 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 423 9 0 3 5.1 CCCCN(C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789386 63146 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 423 9 0 3 5.1 CCCCN(C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
10300661 63157 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 421 9 0 2 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779135 63157 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 421 9 0 2 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789451 63157 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 421 9 0 2 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
117628769 145114 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 772 15 5 13 5.2 CN(CCCn1c(=O)oc2cc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3911114 145114 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 772 15 5 13 5.2 CN(CCCn1c(=O)oc2cc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
54586745 63160 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 523 8 0 2 6.8 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCCc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779138 63160 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 523 8 0 2 6.8 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCCc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1789461 63160 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 523 8 0 2 6.8 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCCc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
688566 198339 None 17 Human Binding pIC50 = 9.1 9.1 - 3
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 337 4 1 4 2.6 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
CHEMBL558910 198339 None 17 Human Binding pIC50 = 9.1 9.1 - 3
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 337 4 1 4 2.6 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
44235871 199028 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 2 1 4 2.5 O=C(O[C@H]1CN2CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL563887 199028 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 2 1 4 2.5 O=C(O[C@H]1CN2CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
44236334 14017 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL1197117 14017 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL559931 14017 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 10.1021/jm900132z
9946010 62360 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 342 4 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779034 62360 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 342 4 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
10208972 63152 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 457 8 0 3 5.5 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779129 63152 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 457 8 0 3 5.5 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789429 63152 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 457 8 0 3 5.5 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
57390714 68791 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 8 0 4 4.9 Cc1cccc(OCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)c1 10.1016/j.bmcl.2011.10.002
CHEMBL1921933 68791 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 8 0 4 4.9 Cc1cccc(OCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)c1 10.1016/j.bmcl.2011.10.002
57395997 68854 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccnn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922049 68854 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccnn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988641 69163 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 359 4 0 3 3.4 CC1CCN(C(C)(C(=O)OC2CC[N+](C)(C)CC2)c2ccccc2)CC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924033 69163 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 359 4 0 3 3.4 CC1CCN(C(C)(C(=O)OC2CC[N+](C)(C)CC2)c2ccccc2)CC1 10.1016/j.bmcl.2011.10.002
57403964 69172 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 385 5 0 3 3.9 CC(C)[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
CHEMBL1924042 69172 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 385 5 0 3 3.9 CC(C)[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
72545782 103692 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 463 7 0 3 6.0 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c(C)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087233 103692 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 463 7 0 3 6.0 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c(C)n1 10.1016/j.bmcl.2013.09.092
72547497 103728 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)ncn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087378 103728 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)ncn1 10.1016/j.bmcl.2013.09.092
71565927 146749 None 0 Human Binding pIC50 = 9 9.0 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 758 12 4 11 6.3 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C2(C)c3ccccc3Oc3ccccc32)CC1 nan
CHEMBL3923686 146749 None 0 Human Binding pIC50 = 9 9.0 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 758 12 4 11 6.3 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C2(C)c3ccccc3Oc3ccccc32)CC1 nan
54672858 151562 None 0 Human Binding pIC50 = 9 9.0 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 794 16 7 12 5.9 COc1cc(NC(=O)CCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3962171 151562 None 0 Human Binding pIC50 = 9 9.0 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 794 16 7 12 5.9 COc1cc(NC(=O)CCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
44233175 14024 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL1197209 14024 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL562655 14024 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
44233173 14025 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL1197216 14025 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL562890 14025 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
23724781 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
23724781.0 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
316 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
317 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
71183 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
CHEMBL1354199 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
CHEMBL3140030 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
CHEMBL376897 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
DB00462 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
10246307 117842 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 4 2 4 2.3 O=C(N[C@H]1CN2CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1016/j.bmcl.2015.02.065
CHEMBL3401643 117842 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 4 2 4 2.3 O=C(N[C@H]1CN2CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1016/j.bmcl.2015.02.065
54590925 153402 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 794 15 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3978112 153402 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 794 15 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
23724781 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 nan
23724781.0 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 nan
316 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 nan
317 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 nan
71183 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 nan
CHEMBL1354199 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 nan
CHEMBL3140030 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 nan
CHEMBL376897 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 nan
DB00462 2835 None 13 Human Binding pIC50 = 9.0 9.0 -2 9
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 nan
9967590 62161 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 336 4 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1777826 62161 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 336 4 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
54582845 63151 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 525 8 0 3 6.2 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCOc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779139 63151 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 525 8 0 3 6.2 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCOc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1789405 63151 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 525 8 0 3 6.2 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCOc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
50925542 19184 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4cccc(Cl)c4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289653 19184 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4cccc(Cl)c4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
57401170 68780 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 8 0 4 4.9 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cn1 10.1016/j.bmcl.2011.10.002
CHEMBL1921922 68780 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 8 0 4 4.9 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cn1 10.1016/j.bmcl.2011.10.002
57397790 68789 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 497 8 0 4 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccc(Cl)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921931 68789 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 497 8 0 4 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccc(Cl)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57402970 68853 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccncn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922048 68853 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccncn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988643 69162 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 381 4 0 3 3.4 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCC(F)(F)CC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924032 69162 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 381 4 0 3 3.4 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCC(F)(F)CC1 10.1016/j.bmcl.2011.10.002
1201549 597 None 17 Human Binding pIC50 = 8.9 8.9 -1 20
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
1201549.0 597 None 17 Human Binding pIC50 = 8.9 8.9 -1 20
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 597 None 17 Human Binding pIC50 = 8.9 8.9 -1 20
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 597 None 17 Human Binding pIC50 = 8.9 8.9 -1 20
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 597 None 17 Human Binding pIC50 = 8.9 8.9 -1 20
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 597 None 17 Human Binding pIC50 = 8.9 8.9 -1 20
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 597 None 17 Human Binding pIC50 = 8.9 8.9 -1 20
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
54592027 144080 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 717 15 5 11 5.3 CN(CCOc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3902803 144080 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 717 15 5 11 5.3 CN(CCOc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
54583840 62371 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 404 4 0 3 4.7 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2CN3CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779045 62371 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 404 4 0 3 4.7 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2CN3CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
118638354 145675 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 17 5 11 5.3 CN(CCN(C)[C@H]1CC[C@H](OC(C(=O)O)(c2cccs2)c2cccs2)CC1)C(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 nan
CHEMBL3915401 145675 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 17 5 11 5.3 CN(CCN(C)[C@H]1CC[C@H](OC(C(=O)O)(c2cccs2)c2cccs2)CC1)C(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 nan
54673189 149250 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 801 15 6 14 5.3 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(C#N)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3943564 149250 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 801 15 6 14 5.3 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(C#N)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
25147683 62372 None 31 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 408 4 0 3 4.5 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779046 62372 None 31 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 408 4 0 3 4.5 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
10372836 102452 None 36 Human Binding pIC50 = 8.8 8.8 - 1
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
CHEMBL3039518 102452 None 36 Human Binding pIC50 = 8.8 8.8 - 1
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
54591014 145858 None 5 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
CHEMBL3916700 145858 None 5 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
71558565 167538 None 10 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 742 14 5 13 5.0 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 10.1021/acs.jmedchem.8b01520
CHEMBL4297483 167538 None 10 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 742 14 5 13 5.0 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 10.1021/acs.jmedchem.8b01520
155531077 171723 None 2 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 669 10 4 10 4.4 CC(C)c1ncc(C(=O)N2CCOC3(CCN(Cc4ccc(F)c(CCNC[C@H](O)c5ccc(O)c6[nH]c(=O)sc56)c4)CC3)C2)s1 10.1021/acs.jmedchem.8b01520
CHEMBL4465556 171723 None 2 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 669 10 4 10 4.4 CC(C)c1ncc(C(=O)N2CCOC3(CCN(Cc4ccc(F)c(CCNC[C@H](O)c5ccc(O)c6[nH]c(=O)sc56)c4)CC3)C2)s1 10.1021/acs.jmedchem.8b01520
57397743 68773 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 486 7 1 3 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3c[nH]c4ccccc34)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921913 68773 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 486 7 1 3 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3c[nH]c4ccccc34)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57393499 71622 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 316 4 0 2 3.5 CC(C(=O)O[C@@H]1CC[N+](C)(C)C1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924026 71622 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 316 4 0 2 3.5 CC(C(=O)O[C@@H]1CC[N+](C)(C)C1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1963231 71622 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 316 4 0 2 3.5 CC(C(=O)O[C@@H]1CC[N+](C)(C)C1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
54591014 145858 None 5 Human Binding pIC50 = 8.8 8.8 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3916700 145858 None 5 Human Binding pIC50 = 8.8 8.8 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
54673020 151675 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 766 14 6 11 5.5 CN(CCC(=O)Nc1cc(F)c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1F)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3963417 151675 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 766 14 6 11 5.5 CN(CCC(=O)Nc1cc(F)c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1F)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
10143954 13624 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL1194286 13624 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL549986 13624 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
11306852 14030 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 434 8 1 3 5.0 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C1(O)c3ccccc3-c3ccccc31)C2 10.1021/jm900132z
CHEMBL1197250 14030 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 434 8 1 3 5.0 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C1(O)c3ccccc3-c3ccccc31)C2 10.1021/jm900132z
CHEMBL563996 14030 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 434 8 1 3 5.0 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C1(O)c3ccccc3-c3ccccc31)C2 10.1021/jm900132z
325 2062 None 10 Human Binding pIC50 = 8.8 8.8 -1 9
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1016/j.bmcl.2015.02.065
3746 2062 None 10 Human Binding pIC50 = 8.8 8.8 -1 9
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1016/j.bmcl.2015.02.065
657308 2062 None 10 Human Binding pIC50 = 8.8 8.8 -1 9
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1016/j.bmcl.2015.02.065
CHEMBL1615433 2062 None 10 Human Binding pIC50 = 8.8 8.8 -1 9
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1016/j.bmcl.2015.02.065
DB00332 2062 None 10 Human Binding pIC50 = 8.8 8.8 -1 9
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 10.1016/j.bmcl.2015.02.065
9944783 62363 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 316 6 0 3 3.9 CCCCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779037 62363 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 316 6 0 3 3.9 CCCCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
54673702 149719 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 814 15 6 14 5.6 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2c1OCC(=O)N2 nan
CHEMBL3947244 149719 None 0 Human Binding pIC50 = 8.8