Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
9815409 12332 22 None 1 2 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1185481 12332 22 None 1 2 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL416736 12332 22 None 1 2 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
1979 77297 70 None -2089 7 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 10.1021/jm960467d
CHEMBL20835 77297 70 None -2089 7 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 10.1021/jm960467d
2551 791 23 None 2 13 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 791 23 None -4 13 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
298 791 23 None -4 13 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
488 791 23 None -4 13 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
CHEMBL965 791 23 None -4 13 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
DB00411 791 23 None -4 13 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
9838581 11945 2 None 4 2 Mouse 6.0 pEC50 = 6.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1183042 11945 2 None 4 2 Mouse 6.0 pEC50 = 6.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL277014 11945 2 None 4 2 Mouse 6.0 pEC50 = 6.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1 10.1021/jm960467d
3652 4066 79 None -1737 15 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
57 4066 79 None -1737 15 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
60809 4066 79 None -1737 15 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
CHEMBL21536 4066 79 None -1737 15 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
DB15357 4066 79 None -1737 15 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
10703031 11118 0 None - 1 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 196 3 1 6 -0.1 COCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1178347 11118 0 None - 1 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 196 3 1 6 -0.1 COCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL22089 11118 0 None - 1 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 196 3 1 6 -0.1 COCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
44589681 185264 0 None -12 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL485913 185264 0 None -12 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
22745278 187039 1 None -53 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL491209 187039 1 None -53 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
306 3430 21 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
3536 3430 21 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
53930639 3430 21 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
9577995 3430 21 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
CHEMBL134641 3430 21 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
3652 4066 79 None -275 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57 4066 79 None -275 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809 4066 79 None -275 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
CHEMBL21536 4066 79 None -275 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
DB15357 4066 79 None -275 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
2551 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
1726 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
7438 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
CHEMBL978 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
DB06709 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
2230 464 60 None -17 9 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
296 464 60 None -17 9 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
CHEMBL7303 464 60 None -17 9 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
DB04365 464 60 None -17 9 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
10375030 13922 0 None - 1 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 4 -0.1 C#CCOC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL1196670 13922 0 None - 1 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 4 -0.1 C#CCOC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL557795 13922 0 None - 1 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 4 -0.1 C#CCOC(=O)C1CCC(N)=NC1 10.1021/jm960467d
2551 791 23 None 2 13 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
650899 54384 11 None -4 5 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1535797 54384 11 None -4 5 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1609153 54384 11 None -4 5 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
42599070 16046 0 None -316 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223804 16046 0 None -316 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598359 16074 0 None -100 5 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223864 16074 0 None -100 5 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
2551 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
9308 17722 21 None 3 9 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL1255785 17722 21 None 3 9 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL12587 17722 21 None 3 9 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL292911 17722 21 None 3 9 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
2551 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
156015300 177568 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640703 177568 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
10012139 13678 11 None 2 2 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL1194965 13678 11 None 2 2 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL553602 13678 11 None 2 2 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1 10.1021/jm960467d
10240891 206075 0 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 140 1 0 3 0.3 CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL85678 206075 0 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 140 1 0 3 0.3 CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
2551 791 23 None 2 13 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 791 23 None -4 13 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
298 791 23 None -4 13 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
488 791 23 None -4 13 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
CHEMBL965 791 23 None -4 13 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
DB00411 791 23 None -4 13 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
42598360 16072 0 None -630 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223862 16072 0 None -630 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
9990434 106312 0 None -3 3 Human 4.8 pEC50 = 4.8 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 202 2 0 3 0.7 C#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL313918 106312 0 None -3 3 Human 4.8 pEC50 = 4.8 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 202 2 0 3 0.7 C#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
156021744 178090 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4648071 178090 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
92209180 13121 7 None 2 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
9793884 13121 7 None 2 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL1190710 13121 7 None 2 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL541398 13121 7 None 2 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
124300908 13162 6 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
2606 13162 6 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL1191029 13162 6 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL542065 13162 6 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
2551 791 23 None -4 13 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
298 791 23 None -4 13 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
488 791 23 None -4 13 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
CHEMBL965 791 23 None -4 13 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
DB00411 791 23 None -4 13 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
156015097 177528 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4640324 177528 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
2551 791 23 None 2 13 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 791 23 None 2 13 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
42598829 16048 0 None -251 5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223806 16048 0 None -251 5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598828 16071 0 None -1584 5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223861 16071 0 None -1584 5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
187 255 39 None -1 8 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
294 255 39 None -1 8 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
65 255 39 None -1 8 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
8593 255 39 None -1 8 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
CHEMBL667 255 39 None -1 8 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
DB03128 255 39 None -1 8 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
2551 791 23 None 2 13 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
71737672 2559 19 None -3 6 Human 5.7 pEC50 = 5.7 Functional
Activity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2559 19 None -3 6 Human 5.7 pEC50 = 5.7 Functional
Activity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2559 19 None -3 6 Human 5.7 pEC50 = 5.7 Functional
Activity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
44158142 188646 43 None -1 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
CHEMBL503735 188646 43 None -1 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
44158142 188646 43 None -1 4 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
CHEMBL503735 188646 43 None -1 4 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
2551 791 23 None -4 13 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
298 791 23 None -4 13 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
488 791 23 None -4 13 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
CHEMBL965 791 23 None -4 13 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
DB00411 791 23 None -4 13 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
16071018 16022 20 None -398 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223753 16022 20 None -398 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
42598357 16073 0 None -794 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223863 16073 0 None -794 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
16071018 16022 20 None -398 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
CHEMBL1223753 16022 20 None -398 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
3652 4066 79 None -275 15 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4066 79 None -275 15 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4066 79 None -275 15 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4066 79 None -275 15 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4066 79 None -275 15 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
71792 78377 38 None -6 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
CHEMBL2111051 78377 38 None -6 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
44251554 7029 0 None -1 4 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory)
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
CHEMBL1084941 7029 0 None -1 4 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory)
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
44422692 11821 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182296 11821 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL228144 11821 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
14235519 16524 8 None 4 2 Mouse 5.6 pEC50 = 5.6 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 179 1 0 4 1.1 Cc1noc(C2=CCCN(C)C2)n1 10.1021/jm960467d
CHEMBL12378 16524 8 None 4 2 Mouse 5.6 pEC50 = 5.6 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 179 1 0 4 1.1 Cc1noc(C2=CCCN(C)C2)n1 10.1021/jm960467d
187 255 39 None -1 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
294 255 39 None -1 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
65 255 39 None -1 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
8593 255 39 None -1 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
CHEMBL667 255 39 None -1 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
DB03128 255 39 None -1 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
187 255 39 None -1 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
294 255 39 None -1 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
65 255 39 None -1 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
8593 255 39 None -1 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
CHEMBL667 255 39 None -1 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
DB03128 255 39 None -1 8 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
9815331 203084 1 None 3 5 Rat 8.4 pEC50 = 8.4 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 203084 1 None 3 5 Rat 8.4 pEC50 = 8.4 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
9883040 100509 0 None -3 3 Human 8.4 pEC50 = 8.4 Functional
In vitro functional agonism against M3 muscarinic receptor (PI)In vitro functional agonism against M3 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL291339 100509 0 None -3 3 Human 8.4 pEC50 = 8.4 Functional
In vitro functional agonism against M3 muscarinic receptor (PI)In vitro functional agonism against M3 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL542622 100509 0 None -3 3 Human 8.4 pEC50 = 8.4 Functional
In vitro functional agonism against M3 muscarinic receptor (PI)In vitro functional agonism against M3 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
2551 791 23 None 2 13 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 791 23 None 2 13 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
71737672 2559 19 None -5 6 Rat 5.5 pEC50 = 5.5 Functional
Activity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2559 19 None -5 6 Rat 5.5 pEC50 = 5.5 Functional
Activity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2559 19 None -5 6 Rat 5.5 pEC50 = 5.5 Functional
Activity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
42599068 16047 0 None -100 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223805 16047 0 None -100 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42599071 16092 0 None -1258 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223939 16092 0 None -1258 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
319 1312 44 None -22 18 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
321 1312 44 None -22 18 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031 1312 44 None -22 18 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
784 1312 44 None -22 18 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
CHEMBL1346 1312 44 None -22 18 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
DB00496 1312 44 None -22 18 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
2551 791 23 None 2 13 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
42598586 16091 0 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223938 16091 0 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25207745 16094 0 None -398 5 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223941 16094 0 None -398 5 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
44253016 80428 2 None -316 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
CHEMBL2146597 80428 2 None -316 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
16123945 80430 12 None -794 5 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
CHEMBL2146599 80430 12 None -794 5 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
156011965 177268 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636528 177268 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
2551 791 23 None 2 13 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
24865895 95976 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL259662 95976 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL390842 95976 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
2551 791 23 None 2 13 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
319 1312 44 None -22 18 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
321 1312 44 None -22 18 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031 1312 44 None -22 18 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
784 1312 44 None -22 18 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
CHEMBL1346 1312 44 None -22 18 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
DB00496 1312 44 None -22 18 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
2551 791 23 None 2 13 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
298 791 23 None 2 13 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
488 791 23 None 2 13 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
CHEMBL965 791 23 None 2 13 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
DB00411 791 23 None 2 13 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
367 3795 12 None -3 8 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
5487427 3795 12 None -3 8 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
8592 3795 12 None -3 8 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL1900528 3795 12 None -3 8 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL3305968 3795 12 None -3 8 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL4650755 3795 12 None -3 8 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
DB01409 3795 12 None -3 8 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
10197743 12913 9 None - 1 Mouse 4.3 pEC50 = 4.3 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
92209179 12913 9 None - 1 Mouse 4.3 pEC50 = 4.3 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL1189286 12913 9 None - 1 Mouse 4.3 pEC50 = 4.3 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL538467 12913 9 None - 1 Mouse 4.3 pEC50 = 4.3 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
2551 791 23 None -4 13 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 791 23 None -4 13 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 791 23 None -4 13 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 791 23 None -4 13 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 791 23 None -4 13 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
44422699 11819 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182272 11819 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL227378 11819 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
44422692 11821 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182296 11821 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL228144 11821 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
10727260 11956 0 None 2 2 Mouse 5.2 pEC50 = 5.2 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1183133 11956 0 None 2 2 Mouse 5.2 pEC50 = 5.2 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL281411 11956 0 None 2 2 Mouse 5.2 pEC50 = 5.2 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
334 236 27 None -144 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 receptor by calcium mobilization assayAgonist activity at human muscarinic M3 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
9928284 236 27 None -144 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 receptor by calcium mobilization assayAgonist activity at human muscarinic M3 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
CHEMBL2022960 236 27 None -144 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 receptor by calcium mobilization assayAgonist activity at human muscarinic M3 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
644390 40382 6 None -2 4 Human 4.2 pEC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
CHEMBL1482157 40382 6 None -2 4 Human 4.2 pEC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
156014812 178238 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4647437 178238 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650736 178238 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
156009673 178230 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4633816 178230 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650683 178230 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
156015300 177568 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640703 177568 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
42598591 16045 0 None -125 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223803 16045 0 None -125 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25230693 16093 0 None -251 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223940 16093 0 None -251 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
3008304 3992 52 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
7632 3992 52 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
CHEMBL523685 3992 52 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
147230103 180129 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
CHEMBL4748915 180129 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
3008304 3992 52 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
7632 3992 52 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
CHEMBL523685 3992 52 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
3008304 3992 52 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
7632 3992 52 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
CHEMBL523685 3992 52 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
2551 791 23 None 2 13 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 791 23 None 2 13 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
135409468 2022 69 None -13 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
333 2022 69 None -13 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
CHEMBL845 2022 69 None -13 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
647412 27288 9 None -5 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
CHEMBL1367424 27288 9 None -5 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
24967746 16023 0 None -199 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223754 16023 0 None -199 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598358 16070 0 None -794 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223860 16070 0 None -794 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
10397133 107035 1 None -3 3 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 164 2 0 3 0.3 C#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL315676 107035 1 None -3 3 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 164 2 0 3 0.3 C#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
10397356 120690 0 None -5 3 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL354738 120690 0 None -5 3 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
10130070 120304 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 154 2 0 3 0.7 CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL352908 120304 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 154 2 0 3 0.7 CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
156011965 177268 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636528 177268 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
2551 791 23 None 2 13 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None 2 13 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None 2 13 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None 2 13 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None 2 13 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
10375322 58700 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 192 2 0 3 1.1 CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL168545 58700 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 192 2 0 3 1.1 CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
2551 791 23 None -93 13 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
298 791 23 None -93 13 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
488 791 23 None -93 13 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
CHEMBL965 791 23 None -93 13 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
DB00411 791 23 None -93 13 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
2551 791 23 None -4 13 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
298 791 23 None -4 13 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
488 791 23 None -4 13 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
CHEMBL965 791 23 None -4 13 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
DB00411 791 23 None -4 13 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
5487543 205623 4 None -41 6 Human 5.4 pED50 = 5.4 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
CHEMBL81878 205623 4 None -41 6 Human 5.4 pED50 = 5.4 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
9795428 96459 5 None -20 5 Human 6.1 pED50 = 6.1 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
CHEMBL262455 96459 5 None -20 5 Human 6.1 pED50 = 6.1 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
11442478 106451 0 None 1 3 Human 9.0 pIC50 = 9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 4 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085073 106451 0 None 1 3 Human 9.0 pIC50 = 9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 4 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140113 106451 0 None 1 3 Human 9.0 pIC50 = 9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 4 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL5074216 214292 0 None - 1 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@@H]3CCN(C)C3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5074599 214296 2 None - 1 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5074216 214292 0 None - 1 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@@H]3CCN(C)C3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5086393 215003 0 None - 1 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44589585 188868 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 10 4 5 4.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL507375 188868 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 10 4 5 4.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555474 188868 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 10 4 5 4.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5074599 214296 2 None - 1 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44232700 106484 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3084399 106484 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3140218 106484 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
11341753 187279 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 8 2 4 4.1 CCOc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492978 187279 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 8 2 4 4.1 CCOc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11341940 187338 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 CC1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493328 187338 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 CC1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
11364721 192700 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 427 7 2 4 3.9 CC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL522020 192700 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 427 7 2 4 3.9 CC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44589495 185956 0 None 10 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 5 7 3.8 CCCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL486982 185956 0 None 10 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 5 7 3.8 CCCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590173 189067 0 None -1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL510029 189067 0 None -1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555019 189067 0 None -1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5076886 214444 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3C[C@H]4CC[C@H](C3)N4C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
71452454 83889 0 None 41 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 603 9 3 7 3.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206587 83889 0 None 41 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 603 9 3 7 3.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2012.09.085
11552174 103474 0 None 1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085090 103474 0 None 1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
11330061 187288 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492997 187288 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2009.01.098
44589570 172733 0 None 15 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 10 5 6 3.5 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL451040 172733 0 None 15 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 10 5 6 3.5 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589498 172734 0 None 3 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 572 11 5 7 3.8 O=C(Nc1ccc(C(=O)OCC2CC2)cc1)N[C@@H](Cc1ccc(O)cc1)C(=O)NC1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL451043 172734 0 None 3 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 572 11 5 7 3.8 O=C(Nc1ccc(C(=O)OCC2CC2)cc1)N[C@@H](Cc1ccc(O)cc1)C(=O)NC1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.09.020
44573500 187696 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1Cl 10.1016/j.bmcl.2009.01.098
CHEMBL495361 187696 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1Cl 10.1016/j.bmcl.2009.01.098
44589575 175619 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 596 9 4 7 2.9 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)N4CCOCC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL458105 175619 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 596 9 4 7 2.9 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)N4CCOCC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
145955917 162459 0 None -29 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 418 6 2 4 4.2 NC[C@H]1CC[C@H](CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
CHEMBL4167221 162459 0 None -29 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 418 6 2 4 4.2 NC[C@H]1CC[C@H](CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
44233187 85996 0 None -2 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2306159 85996 0 None -2 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233187 85996 0 None -2 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2306159 85996 0 None -2 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
76324336 103470 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085086 103470 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
76331543 103476 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 4 4.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085092 103476 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 4 4.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
57758637 106472 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 441 7 0 1 7.2 C[N+]1(CCC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084466 106472 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 441 7 0 1 7.2 C[N+]1(CCC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140183 106472 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 441 7 0 1 7.2 C[N+]1(CCC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44232702 106476 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3084401 106476 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3140203 106476 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
11547053 106438 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 3 5.0 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085074 106438 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 3 5.0 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140097 106438 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 3 5.0 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
145958296 162258 0 None -38 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4164075 162258 0 None -38 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
142416754 162318 0 None -112 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 480 8 2 4 5.2 FC1(F)CCC(NC/C=C\CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
CHEMBL4164874 162318 0 None -112 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 480 8 2 4 5.2 FC1(F)CCC(NC/C=C\CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
44232708 106459 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cc(F)cc(F)c1)c1cc(F)cc(F)c1)C2 10.1021/jm900736e
CHEMBL3084407 106459 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cc(F)cc(F)c1)c1cc(F)cc(F)c1)C2 10.1021/jm900736e
CHEMBL3140145 106459 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cc(F)cc(F)c1)c1cc(F)cc(F)c1)C2 10.1021/jm900736e
76320693 103466 0 None 1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085082 103466 0 None 1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
76309756 103467 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 375 4 0 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085083 103467 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 375 4 0 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44590174 170033 0 None -3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 651 10 3 6 4.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Br)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL444300 170033 0 None -3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 651 10 3 6 4.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Br)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL466271 170033 0 None -3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 651 10 3 6 4.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Br)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590177 188898 0 None -5 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 677 12 3 7 5.1 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(=O)c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL507874 188898 0 None -5 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 677 12 3 7 5.1 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(=O)c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL554918 188898 0 None -5 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 677 12 3 7 5.1 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(=O)c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5076535 214422 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCCN(C)C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
11699452 12589 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 456 8 1 2 5.8 Cc1ccc(C(O)(c2ccc(C)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1187080 12589 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 456 8 1 2 5.8 Cc1ccc(C(O)(c2ccc(C)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL489626 12589 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 456 8 1 2 5.8 Cc1ccc(C(O)(c2ccc(C)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
44590179 172693 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccccc2Cl)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450538 172693 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccccc2Cl)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL553446 172693 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccccc2Cl)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44573621 187188 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 477 8 2 4 5.5 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492391 187188 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 477 8 2 4 5.5 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2009.01.098
44573263 193126 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CN2CCNCC2)cc1-c1cccc(CNC(=O)c2ccc3c(c2)OCO3)c1 10.1016/j.bmcl.2009.01.098
CHEMBL522992 193126 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CN2CCNCC2)cc1-c1cccc(CNC(=O)c2ccc3c(c2)OCO3)c1 10.1016/j.bmcl.2009.01.098
44590181 173540 0 None -25 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 633 12 3 8 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)c(OC)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL453248 173540 0 None -25 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 633 12 3 8 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)c(OC)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL551113 173540 0 None -25 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 633 12 3 8 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)c(OC)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
162646559 179616 0 None -97 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@@H](C)C1 10.1021/acsmedchemlett.0c00626
CHEMBL4742997 179616 0 None -97 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@@H](C)C1 10.1021/acsmedchemlett.0c00626
71459724 83978 0 None 63 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2207177 83978 0 None 63 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
42626092 12603 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187132 12603 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL491246 12603 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
145956824 162237 0 None -1412 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.1 NCC1CC1CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4163770 162237 0 None -1412 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.1 NCC1CC1CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
44233417 86017 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2307674 86017 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233417 86017 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2307674 86017 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
76324303 103222 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.6 CN1[C@H]2CC[C@@H]1C[C@H](CCC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084394 103222 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.6 CN1[C@H]2CC[C@@H]1C[C@H](CCC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
76327870 103225 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 273 4 1 2 3.5 CCC(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1021/jm900736e
CHEMBL3084397 103225 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 273 4 1 2 3.5 CCC(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1021/jm900736e
76327903 103477 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 381 4 0 5 4.4 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085093 103477 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 381 4 0 5 4.4 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
76316969 106496 0 None -2 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 396 4 0 4 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(C#N)c1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085075 106496 0 None -2 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 396 4 0 4 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(C#N)c1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140262 106496 0 None -2 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 396 4 0 4 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(C#N)c1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
71455969 83901 0 None 3 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 581 12 4 5 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206603 83901 0 None 3 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 581 12 4 5 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
1765112 103221 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 307 3 1 2 3.8 CN1[C@H]2CC[C@@H]1C[C@H](C(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084393 103221 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 307 3 1 2 3.8 CN1[C@H]2CC[C@@H]1C[C@H](C(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
25034111 193394 0 None 7 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL526009 193394 0 None 7 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
16040727 169419 0 None -3 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 649 11 3 6 5.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL442672 169419 0 None -3 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 649 11 3 6 5.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL495102 169419 0 None -3 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 649 11 3 6 5.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590124 169770 0 None 39 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 4 6 4.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL443925 169770 0 None 39 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 4 6 4.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590172 170294 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 591 10 3 6 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL444688 170294 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 591 10 3 6 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL527216 170294 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 591 10 3 6 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590171 178724 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 587 10 3 6 4.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL468609 178724 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 587 10 3 6 4.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL554632 178724 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 587 10 3 6 4.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590125 183837 0 None 12 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 530 10 4 6 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL480878 183837 0 None 12 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 530 10 4 6 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590170 188347 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 4 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL501348 188347 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 4 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL553431 188347 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 4 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
25034111 193394 0 None 7 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL526009 193394 0 None 7 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
76309754 106494 0 None -1 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085062 106494 0 None -1 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
CHEMBL3140260 106494 0 None -1 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
44589571 172563 0 None 10 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 580 11 5 6 3.5 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCC4CC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL448904 172563 0 None 10 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 580 11 5 6 3.5 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCC4CC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
71452456 83907 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 525 10 4 5 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(C)CCCCCC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206609 83907 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 525 10 4 5 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(C)CCCCCC2)cc1 10.1016/j.bmcl.2012.09.085
25034180 188388 0 None -1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL502000 188388 0 None -1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
44573744 187625 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 7 1 5 4.2 CCN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL494996 187625 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 7 1 5 4.2 CCN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44589573 188881 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 616 11 5 6 4.3 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL507581 188881 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 616 11 5 6 4.3 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
11510358 106457 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 355 4 0 3 4.2 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085069 106457 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 355 4 0 3 4.2 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140143 106457 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 355 4 0 3 4.2 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44232947 106442 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccsc1)c1ccsc1)C2 10.1021/jm900736e
CHEMBL3084411 106442 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccsc1)c1ccsc1)C2 10.1021/jm900736e
CHEMBL3140100 106442 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccsc1)c1ccsc1)C2 10.1021/jm900736e
11664153 12725 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1cccc(C(O)(c2cccc(OC)c2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL1187845 12725 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1cccc(C(O)(c2cccc(OC)c2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL523767 12725 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1cccc(C(O)(c2cccc(OC)c2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
76324304 103223 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 322 4 1 3 3.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccn1)C2 10.1021/jm900736e
CHEMBL3084395 103223 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 322 4 1 3 3.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccn1)C2 10.1021/jm900736e
15945874 188741 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL505452 188741 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
44573578 187183 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 7 2 5 3.5 COC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492374 187183 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 7 2 5 3.5 COC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11455956 187577 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 463 7 2 5 3.1 CS(=O)(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494749 187577 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 463 7 2 5 3.1 CS(=O)(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44590033 183654 0 None 12 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL480299 183654 0 None 12 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
15945874 188741 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL505452 188741 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589984 190534 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL518001 190534 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
1201549 594 24 None -4 26 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
333 594 24 None -4 26 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
7601 594 24 None -4 26 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
CHEMBL1201203 594 24 None -4 26 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
CHEMBL438151 594 24 None -4 26 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
DB00245 594 24 None -4 26 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
CHEMBL5076445 214418 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CCN3C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5078006 214505 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5086393 215003 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44232953 103364 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
CHEMBL3084663 103364 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
44232953 103364 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
CHEMBL3084663 103364 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
71459689 83887 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 595 13 4 5 5.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206585 83887 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 595 13 4 5 5.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
44573264 187178 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2ccc(F)c(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL492359 187178 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2ccc(F)c(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44573619 187578 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 7 3 4 3.6 CC(=O)Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494752 187578 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 7 3 4 3.6 CC(=O)Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11714747 187609 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 7 2 4 3.8 CN(C)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494950 187609 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 7 2 4 3.8 CN(C)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11578568 187610 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 400 6 3 4 3.3 Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494951 187610 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 400 6 3 4 3.3 Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44573661 188357 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 401 6 3 4 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(O)c1 10.1016/j.bmcl.2009.01.098
CHEMBL501486 188357 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 401 6 3 4 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(O)c1 10.1016/j.bmcl.2009.01.098
25034112 188369 0 None -1 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL501727 188369 0 None -1 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
11690968 106474 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085072 106474 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140185 106474 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
11518068 106479 0 None 1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085059 106479 0 None 1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140213 106479 0 None 1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
11583262 106470 0 None -1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085060 106470 0 None -1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140181 106470 0 None -1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
69444105 103460 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085077 103460 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44233675 103351 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084639 103351 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233675 103351 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084639 103351 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
11712408 106495 0 None -1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
CHEMBL3085067 106495 0 None -1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
CHEMBL3140261 106495 0 None -1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
76327901 103468 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 380 5 0 4 4.5 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
CHEMBL3085084 103468 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 380 5 0 4 4.5 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
11508710 103473 0 None 1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085089 103473 0 None 1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
42626088 12592 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
CHEMBL1187091 12592 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
CHEMBL490236 12592 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
71450615 83902 0 None 1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 609 14 4 5 5.5 CC[N+](CC)(CCNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)Nc1ccc(C(=O)OC(C)C)cc1)Cc1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206604 83902 0 None 1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 609 14 4 5 5.5 CC[N+](CC)(CCNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)Nc1ccc(C(=O)OC(C)C)cc1)Cc1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.085
44232951 106443 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 378 4 1 1 5.3 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CCC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3084416 106443 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 378 4 1 1 5.3 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CCC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3140101 106443 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 378 4 1 1 5.3 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CCC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
10092649 193049 56 None -29 11 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 193049 56 None -29 11 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
145954567 162482 0 None -100 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 416 6 2 4 4.3 NCC1=C(CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CCCC1 10.1021/acsmedchemlett.7b00406
CHEMBL4167521 162482 0 None -100 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 416 6 2 4 4.3 NCC1=C(CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CCCC1 10.1021/acsmedchemlett.7b00406
76324335 103465 0 None -1 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085081 103465 0 None -1 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
10092649 193049 56 None -29 11 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 193049 56 None -29 11 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
71450617 83908 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 527 12 4 5 4.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206610 83908 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 527 12 4 5 4.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2012.09.085
44455159 97737 0 None -20 5 Rat 4.6 pIC50 = 4.6 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 383 5 1 3 4.2 CCN1CCN(c2ccc(NC(=O)[C@H]3C[C@@H]3c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL271704 97737 0 None -20 5 Rat 4.6 pIC50 = 4.6 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 383 5 1 3 4.2 CCN1CCN(c2ccc(NC(=O)[C@H]3C[C@@H]3c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
44234432 106458 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(Cl)c1)c1cccc(Cl)c1)C2 10.1021/jm900736e
CHEMBL3084402 106458 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(Cl)c1)c1cccc(Cl)c1)C2 10.1021/jm900736e
CHEMBL3140144 106458 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(Cl)c1)c1cccc(Cl)c1)C2 10.1021/jm900736e
44590180 172622 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 5.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL449640 172622 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 5.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540398 172622 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 5.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590167 179000 0 None 3 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 494 10 4 6 2.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL471214 179000 0 None 3 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 494 10 4 6 2.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590182 183127 0 None 12 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 532 9 5 7 3.0 COC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL479526 183127 0 None 12 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 532 9 5 7 3.0 COC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590034 189953 0 None 12 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(OC)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL517087 189953 0 None 12 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(OC)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
44573370 187424 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cc(-c2cccc(CN3CCNCC3)c2)ccc1F)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL493939 187424 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cc(-c2cccc(CN3CCNCC3)c2)ccc1F)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44573662 187503 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 399 6 2 3 4.0 Cc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494410 187503 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 399 6 2 3 4.0 Cc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44573420 187585 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 465 7 2 6 3.0 O=S(=O)(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494778 187585 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 465 7 2 6 3.0 O=S(=O)(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44589497 175269 0 None 5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 574 11 5 7 4.0 CC(C)COC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL457302 175269 0 None 5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 574 11 5 7 4.0 CC(C)COC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
11285415 187177 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 458 6 1 4 3.9 C[N+]1(C)CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL492358 187177 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 458 6 1 4 3.9 C[N+]1(C)CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL538863 187177 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 458 6 1 4 3.9 C[N+]1(C)CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44573372 193266 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1F)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL524031 193266 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1F)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44589499 191817 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 540 9 5 6 2.7 CNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL519893 191817 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 540 9 5 6 2.7 CNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
11442669 74250 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2023761 74250 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
76320694 103469 0 None 1 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
CHEMBL3085085 103469 0 None 1 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
11617374 103461 0 None 2 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085078 103461 0 None 2 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
71455965 83891 0 None 3 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](Cc3ccc(Cl)cc3)(C(C)C)CC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206589 83891 0 None 3 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](Cc3ccc(Cl)cc3)(C(C)C)CC2)cc1 10.1016/j.bmcl.2012.09.085
44234194 103369 0 None -1 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 412 7 1 3 3.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(C)(=O)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084670 103369 0 None -1 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 412 7 1 3 3.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(C)(=O)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44234194 103369 0 None -1 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 412 7 1 3 3.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(C)(=O)=O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084670 103369 0 None -1 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 412 7 1 3 3.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(C)(=O)=O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
9044803 124079 11 None -1 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633650 124079 11 None -1 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
9044803 124079 11 None -1 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633650 124079 11 None -1 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
44233419 103372 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 6 1 2 4.4 CC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
CHEMBL3084674 103372 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 6 1 2 4.4 CC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
44233419 103372 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 6 1 2 4.4 CC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
CHEMBL3084674 103372 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 6 1 2 4.4 CC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
44232710 106467 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(F)c(F)c1)c1ccc(F)c(F)c1)C2 10.1021/jm900736e
CHEMBL3084408 106467 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(F)c(F)c1)c1ccc(F)c(F)c1)C2 10.1021/jm900736e
CHEMBL3140173 106467 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(F)c(F)c1)c1ccc(F)c(F)c1)C2 10.1021/jm900736e
11503336 106487 0 None -1 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085071 106487 0 None -1 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140242 106487 0 None -1 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1cccs1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL5078006 214505 0 None - 1 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
11557048 187629 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 497 8 2 5 3.4 CN1CCN(Cc2cccc(C(=O)NCc3cccc(-c4cccc(CN5CCNCC5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL495028 187629 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 497 8 2 5 3.4 CN1CCN(Cc2cccc(C(=O)NCc3cccc(-c4cccc(CN5CCNCC5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
11633399 12587 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 352 6 1 2 3.6 COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187077 12587 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 352 6 1 2 3.6 COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL489225 12587 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 352 6 1 2 3.6 COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
11318734 187306 0 None 5 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 6 2 5 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL493079 187306 0 None 5 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 6 2 5 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
11273131 193105 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)OCO3)cc1-c1cccc(CN2CCNCC2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL522838 193105 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CNC(=O)c2ccc3c(c2)OCO3)cc1-c1cccc(CN2CCNCC2)c1 10.1016/j.bmcl.2009.01.098
44590036 188353 0 None 6 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 574 10 4 8 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL501419 188353 0 None 6 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 574 10 4 8 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590176 189041 0 None -3 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 4.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(F)(F)F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL509614 189041 0 None -3 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 4.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(F)(F)F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555707 189041 0 None -3 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 641 10 3 6 4.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(F)(F)F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
24882532 95088 0 None -7 4 Rat 5.5 pIC50 = 5.5 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL255523 95088 0 None -7 4 Rat 5.5 pIC50 = 5.5 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
44573265 187241 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(-c2cccc(CNC(=O)c3ccc4c(c3)OCO4)c2)cc1CN1CCNCC1 10.1016/j.bmcl.2009.01.098
CHEMBL492756 187241 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(-c2cccc(CNC(=O)c3ccc4c(c3)OCO4)c2)cc1CN1CCNCC1 10.1016/j.bmcl.2009.01.098
44573501 187289 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.01.098
CHEMBL492998 187289 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.01.098
44573663 187504 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 413 7 2 3 4.3 CCc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494411 187504 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 413 7 2 3 4.3 CCc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11421571 187593 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 O=C(NCc1cccc(-c2cccc(CN3CCCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494836 187593 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 O=C(NCc1cccc(-c2cccc(CN3CCCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44573423 187628 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1ccccc1C(=O)NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL495025 187628 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1ccccc1C(=O)NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1 10.1016/j.bmcl.2009.01.098
44589529 186496 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 554 10 5 6 3.1 CCNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL487764 186496 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 554 10 5 6 3.1 CCNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
25034110 188742 0 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL505453 188742 0 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
11584660 93239 8 None -19 5 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human muscarinic receptor M3Antagonist activity at human muscarinic receptor M3
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
CHEMBL244946 93239 8 None -19 5 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human muscarinic receptor M3Antagonist activity at human muscarinic receptor M3
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
44573371 187463 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.7 Cc1ccc(-c2cccc(CN3CCNCC3)c2)cc1CNC(=O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494131 187463 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.7 Cc1ccc(-c2cccc(CN3CCNCC3)c2)cc1CNC(=O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
57758634 106436 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 421 6 0 1 6.5 C[N+]1(Cc2ccccc2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084465 106436 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 421 6 0 1 6.5 C[N+]1(Cc2ccccc2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140095 106436 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 421 6 0 1 6.5 C[N+]1(Cc2ccccc2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11431874 74252 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2023763 74252 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
145958111 161991 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21)CN 10.1021/acsmedchemlett.7b00406
CHEMBL4159607 161991 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21)CN 10.1021/acsmedchemlett.7b00406
71463136 83906 0 None 2 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 12 4 5 5.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(Cc3ccc(Cl)cc3)CCCCC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206608 83906 0 None 2 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 12 4 5 5.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(Cc3ccc(Cl)cc3)CCCCC2)cc1 10.1016/j.bmcl.2012.09.085
76320690 106433 0 None -1 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085063 106433 0 None -1 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140092 106433 0 None -1 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccc(Br)c1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
6908726 108938 5 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Agonist activity at endothelial M3 receptor in Wistar-Kyoto rat thoracic aortic rings assessed as inhibition of phenylephrine-induced contractionAgonist activity at endothelial M3 receptor in Wistar-Kyoto rat thoracic aortic rings assessed as inhibition of phenylephrine-induced contraction
ChEMBL 274 3 1 5 2.2 O=C(N/N=C/c1ccsc1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2018.07.015
CHEMBL3211778 108938 5 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Agonist activity at endothelial M3 receptor in Wistar-Kyoto rat thoracic aortic rings assessed as inhibition of phenylephrine-induced contractionAgonist activity at endothelial M3 receptor in Wistar-Kyoto rat thoracic aortic rings assessed as inhibition of phenylephrine-induced contraction
ChEMBL 274 3 1 5 2.2 O=C(N/N=C/c1ccsc1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2018.07.015
42626096 12713 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1ccc(C(O)(c2ccc(OC)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1187802 12713 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1ccc(C(O)(c2ccc(OC)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL521921 12713 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1ccc(C(O)(c2ccc(OC)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
137647734 157822 0 None -2 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 448 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4083681 157822 0 None -2 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 448 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
44234683 106477 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1ccc(F)cc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cc(F)ccc1C 10.1021/jm900736e
CHEMBL3084406 106477 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1ccc(F)cc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cc(F)ccc1C 10.1021/jm900736e
CHEMBL3140205 106477 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1ccc(F)cc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cc(F)ccc1C 10.1021/jm900736e
46830361 7859 0 None -10 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 433 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3c(F)c(F)c(F)c(F)c3F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090094 7859 0 None -10 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 433 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3c(F)c(F)c(F)c(F)c3F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
137637944 155791 0 None -3 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4059829 155791 0 None -3 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
11364984 187237 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 444 6 2 6 3.2 C[C@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)n2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL492701 187237 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 444 6 2 6 3.2 C[C@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)n2)CCN1 10.1016/j.bmcl.2009.01.098
44590169 188219 0 None -7 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 603 11 3 7 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL499565 188219 0 None -7 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 603 11 3 7 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL539885 188219 0 None -7 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 603 11 3 7 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
11606547 12568 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 484 8 1 2 6.4 CC(C)(C)c1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1186941 12568 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 484 8 1 2 6.4 CC(C)(C)c1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL483253 12568 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 484 8 1 2 6.4 CC(C)(C)c1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
71463134 83895 0 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 618 11 3 6 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N(C)Cc2n(C)cc[n+]2Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206594 83895 0 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 618 11 3 6 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N(C)Cc2n(C)cc[n+]2Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
44589574 172664 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 582 11 4 6 3.9 CCN(CC)C(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450093 172664 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 582 11 4 6 3.9 CCN(CC)C(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44573543 187465 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1C(F)(F)F 10.1016/j.bmcl.2009.01.098
CHEMBL494151 187465 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1C(F)(F)F 10.1016/j.bmcl.2009.01.098
11399125 193129 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 471 6 1 5 3.7 CC(=O)N1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL523012 193129 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 471 6 1 5 3.7 CC(=O)N1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
11619198 106464 0 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 365 4 0 2 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085058 106464 0 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 365 4 0 2 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140170 106464 0 None -1 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 365 4 0 2 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
137655063 158949 0 None -3 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096143 158949 0 None -3 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccccc3F)ncn2)CC1)N1CCc2ccccc2C1 10.1016/j.bmcl.2017.04.009
76313454 106480 0 None 1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085064 106480 0 None 1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140214 106480 0 None 1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
122195453 124084 0 None -2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633663 124084 0 None -2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
71450662 83977 0 None -1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 611 13 4 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2207176 83977 0 None -1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 611 13 4 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2012.09.085
122195446 124083 0 None -1 5 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
CHEMBL3633656 124083 0 None -1 5 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
76324334 106450 0 None -2 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 369 4 0 3 4.5 Cc1ccoc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085070 106450 0 None -2 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 369 4 0 3 4.5 Cc1ccoc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3140112 106450 0 None -2 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 369 4 0 3 4.5 Cc1ccoc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
46830362 7862 0 None -8 5 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)ccc3C(F)(F)F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090097 7862 0 None -8 5 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)ccc3C(F)(F)F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
76327902 103472 0 None -1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 354 4 0 4 4.4 Cc1ccoc1CN(C(=O)O[C@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085088 103472 0 None -1 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 354 4 0 4 4.4 Cc1ccoc1CN(C(=O)O[C@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
46883796 7861 0 None -1 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 411 4 1 3 4.8 CCN1CCN(c2ccc(NC(=O)c3cccc(C(F)(F)F)c3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090096 7861 0 None -1 4 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 411 4 1 3 4.8 CCN1CCN(c2ccc(NC(=O)c3cccc(C(F)(F)F)c3)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
71463135 83905 0 None 2 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 607 12 4 5 5.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(Cc3ccc(Cl)cc3)CCCC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206607 83905 0 None 2 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 607 12 4 5 5.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(Cc3ccc(Cl)cc3)CCCC2)cc1 10.1016/j.bmcl.2012.09.085
71455968 83897 0 None 2 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206599 83897 0 None 2 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
11168935 187339 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 C[C@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493329 187339 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 C[C@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
44589496 185957 0 None 15 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 10 5 7 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL486983 185957 0 None 15 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 10 5 7 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5076445 214418 0 None - 1 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CCN3C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5081816 214747 0 None - 1 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
11215075 187313 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 C[C@@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493131 187313 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 C[C@@H]1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
11410490 187575 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494741 187575 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.01.098
11249473 187658 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL495172 187658 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44590175 188608 0 None -3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 3 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL503025 188608 0 None -3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 3 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL553433 188608 0 None -3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 3 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590035 191730 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3OC)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL519760 191730 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3OC)C2)cc1 10.1016/j.bmcl.2008.09.020
152278786 182728 1 None -30 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
CHEMBL4790083 182728 1 None -30 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
71452455 83890 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 565 9 3 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(CC3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206588 83890 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 565 9 3 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(CC3CCCCC3)CC2)cc1 10.1016/j.bmcl.2012.09.085
44573305 187238 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 449 6 2 6 3.9 C[C@H]1CN(Cc2ccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)s2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL492702 187238 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 449 6 2 6 3.9 C[C@H]1CN(Cc2ccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)s2)CCN1 10.1016/j.bmcl.2009.01.098
11398832 187587 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 1 5 3.8 CN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL494781 187587 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 1 5 3.8 CN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44573620 187611 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 469 7 2 4 4.6 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494953 187611 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 469 7 2 4 4.6 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2009.01.098
44573499 187695 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1ccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)cc1 10.1016/j.bmcl.2009.01.098
CHEMBL495360 187695 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1ccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)cc1 10.1016/j.bmcl.2009.01.098
44573466 193288 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1ccccc1C(=O)NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL524168 193288 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1ccccc1C(=O)NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1 10.1016/j.bmcl.2009.01.098
44589569 172708 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 11 5 6 3.5 CCCNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450685 172708 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 11 5 6 3.5 CCCNC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589572 188961 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 602 10 5 6 4.6 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)Nc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL508556 188961 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 602 10 5 6 4.6 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)Nc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
162657046 180819 0 None -79 4 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@H](C)C1 10.1021/acsmedchemlett.0c00626
CHEMBL4757103 180819 0 None -79 4 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@H](C)C1 10.1021/acsmedchemlett.0c00626
44573786 187285 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 5 2 5 3.1 O=C(NCc1cccc(-c2cccc(C(=O)N3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL492989 187285 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 5 2 5 3.1 O=C(NCc1cccc(-c2cccc(C(=O)N3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
71454215 83896 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 714 13 4 6 6.5 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCc2n(Cc3ccc(Cl)cc3)cc[n+]2Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206595 83896 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 714 13 4 6 6.5 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCc2n(Cc3ccc(Cl)cc3)cc[n+]2Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
122195454 124086 0 None -8 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633665 124086 0 None -8 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
122195453 124084 0 None -2 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633663 124084 0 None -2 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
10092649 193049 56 None -69 11 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 193049 56 None -69 11 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
10092649 193049 56 None -69 11 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 193049 56 None -69 11 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
152278786 182728 1 None -30 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
CHEMBL4790083 182728 1 None -30 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
76327900 106456 0 None -1 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085061 106456 0 None -1 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140142 106456 0 None -1 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 443 4 0 2 5.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
3156646 8232 9 None -6 3 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 4 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3OC)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1092460 8232 9 None -6 3 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 4 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3OC)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
76309757 103471 0 None 1 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 340 4 0 4 4.0 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085087 103471 0 None 1 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 340 4 0 4 4.0 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
122195446 124083 0 None -1 5 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
CHEMBL3633656 124083 0 None -1 5 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
71454217 83899 0 None -1 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 551 9 3 5 4.3 CC[N+]1(C2CCN(C(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)CC2)CCCC1 10.1016/j.bmcl.2012.09.085
CHEMBL2206601 83899 0 None -1 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 551 9 3 5 4.3 CC[N+]1(C2CCN(C(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)CC2)CCCC1 10.1016/j.bmcl.2012.09.085
122195454 124086 0 None -8 2 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633665 124086 0 None -8 2 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as inhibition of carbachol-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
71450616 83904 0 None 2 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 591 11 4 5 4.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)C23CC4CC(CC(C4)C2)C3)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206606 83904 0 None 2 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 591 11 4 5 4.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)C23CC4CC(CC(C4)C2)C3)cc1 10.1016/j.bmcl.2012.09.085
11284402 192691 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1ccc(F)c(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL521986 192691 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1ccc(F)c(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44589583 172457 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 561 10 5 6 3.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL448294 172457 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 561 10 5 6 3.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555471 172457 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 561 10 5 6 3.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590168 172705 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450652 172705 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540399 172705 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44589584 188755 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 563 10 4 5 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL505651 188755 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 563 10 4 5 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540144 188755 0 None 6 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 563 10 4 5 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590122 192536 0 None 15 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 555 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C#N)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL521244 192536 0 None 15 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 555 10 4 7 3.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C#N)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
11626847 106449 0 None -1 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085068 106449 0 None -1 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3140111 106449 0 None -1 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.071
137655938 158960 0 None -64 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 362 6 2 4 3.0 NC/C=C\CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4096305 158960 0 None -64 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 362 6 2 4 3.0 NC/C=C\CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL5081816 214747 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44573785 187283 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 6 1 5 4.2 CN1CCCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL492987 187283 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 6 1 5 4.2 CN1CCCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44573544 193215 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2009.01.098
CHEMBL523712 193215 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 453 6 2 3 4.7 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2009.01.098
44573421 187586 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 5 2 5 3.7 O=C(Nc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494779 187586 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 5 2 5 3.7 O=C(Nc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44573745 187626 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 6 1 4 5.0 O=C(NCc1cccc(-c2cccc(CN3CCCCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494997 187626 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 6 1 4 5.0 O=C(NCc1cccc(-c2cccc(CN3CCCCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
58975257 103350 0 None -1 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 377 6 2 2 3.9 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(N)=O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084638 103350 0 None -1 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 377 6 2 2 3.9 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(N)=O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
57758619 106465 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 499 15 0 1 9.2 CCCCCCCCCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084469 106465 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 499 15 0 1 9.2 CCCCCCCCCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140171 106465 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 499 15 0 1 9.2 CCCCCCCCCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44232706 106439 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1c(F)cccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cccc(F)c1C 10.1021/jm900736e
CHEMBL3084405 106439 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1c(F)cccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cccc(F)c1C 10.1021/jm900736e
CHEMBL3140098 106439 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 400 4 1 1 5.2 Cc1c(F)cccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1cccc(F)c1C 10.1021/jm900736e
44234686 106452 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 4 1 3 5.1 Cc1cc(C(O)(C[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2csc(C)c2)cs1 10.1021/jm900736e
CHEMBL3084412 106452 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 4 1 3 5.1 Cc1cc(C(O)(C[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2csc(C)c2)cs1 10.1021/jm900736e
CHEMBL3140114 106452 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 376 4 1 3 5.1 Cc1cc(C(O)(C[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2csc(C)c2)cs1 10.1021/jm900736e
137654353 158992 0 None -1 6 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096589 158992 0 None -1 6 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M3 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
71457770 83898 0 None 1 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 647 10 3 5 6.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC([N+]3(Cc4ccc(Cl)cc4)CCCC3)CC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206600 83898 0 None 1 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 647 10 3 5 6.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC([N+]3(Cc4ccc(Cl)cc4)CCCC3)CC2)cc1 10.1016/j.bmcl.2012.09.085
44233189 103374 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 349 5 1 2 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084678 103374 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 349 5 1 2 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233189 103374 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 349 5 1 2 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084678 103374 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 349 5 1 2 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
11602980 103475 0 None 1 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 5 4.6 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085091 103475 0 None 1 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 5 4.6 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
44590178 172714 0 None -1 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2cccc(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450781 172714 0 None -1 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2cccc(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540400 172714 0 None -1 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2cccc(Cl)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590123 183836 0 None 15 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 564 10 4 6 4.3 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(Cl)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL480877 183836 0 None 15 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 564 10 4 6 4.3 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(Cl)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
71457771 83900 0 None 5 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 691 14 4 5 7.0 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(Cc2ccc(Cl)cc2)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206602 83900 0 None 5 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 691 14 4 5 7.0 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(Cc2ccc(Cl)cc2)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
52176747 159007 1 None -16 8 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
CHEMBL4096727 159007 1 None -16 8 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1 10.1016/j.bmcl.2017.05.042
2986945 95026 7 None -63 5 Rat 4.2 pIC50 = 4.2 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 371 6 1 3 4.1 CCN1CCN(c2ccc(NC(=O)CCc3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL255169 95026 7 None -63 5 Rat 4.2 pIC50 = 4.2 Functional
Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M3 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 371 6 1 3 4.1 CCN1CCN(c2ccc(NC(=O)CCc3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
76320692 106481 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 390 4 0 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085065 106481 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 390 4 0 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140215 106481 0 None -2 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 390 4 0 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
76309755 103462 0 None 1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085079 103462 0 None 1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccc(Br)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44234681 106466 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C2 10.1021/jm900736e
CHEMBL3084404 106466 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C2 10.1021/jm900736e
CHEMBL3140172 106466 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 404 4 1 1 5.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccc(Cl)cc1)c1ccc(Cl)cc1)C2 10.1021/jm900736e
76316970 103459 0 None 2 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 350 4 0 3 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085076 103459 0 None 2 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 350 4 0 3 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
145960175 162104 0 None -27 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN)=C(\F)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4161528 162104 0 None -27 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN)=C(\F)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
76313457 103464 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 380 5 0 4 4.5 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085080 103464 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 380 5 0 4 4.5 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
137638270 156853 0 None -6 5 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4071900 156853 0 None -6 5 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
44573465 187250 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1ccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)cc1 10.1016/j.bmcl.2009.01.098
CHEMBL492802 187250 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 410 6 2 4 3.6 N#Cc1ccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)cc1 10.1016/j.bmcl.2009.01.098
11410317 187284 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 441 6 2 5 3.6 O=C(NCc1cccc(-c2cccc(CN3C[C@@H]4C[C@H]3CN4)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL492988 187284 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 441 6 2 5 3.6 O=C(NCc1cccc(-c2cccc(CN3C[C@@H]4C[C@H]3CN4)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
11443944 187660 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL495180 187660 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 7 2 4 3.7 COc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL5076535 214422 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCCN(C)C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44573545 187576 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 403 6 2 3 3.8 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(F)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494742 187576 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 403 6 2 3 3.8 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(F)c1 10.1016/j.bmcl.2009.01.098
44590166 189392 0 None 3 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 468 9 4 6 2.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(CC)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL513228 189392 0 None 3 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 468 9 4 6 2.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(CC)C2)cc1 10.1016/j.bmcl.2008.09.020
44573422 187614 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 444 6 3 5 3.8 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL494962 187614 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 444 6 3 5 3.8 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
71459691 83903 0 None -5 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 723 14 4 5 8.0 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(Cc2ccc3ccccc3c2)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206605 83903 0 None -5 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 723 14 4 5 8.0 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(Cc2ccc3ccccc3c2)Cc2ccc3ccccc3c2)cc1 10.1016/j.bmcl.2012.09.085
1090202 8459 11 None 1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 377 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3ccccc3Cl)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1094003 8459 11 None 1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 377 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3ccccc3Cl)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
44233928 86045 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 438 7 1 2 5.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2308786 86045 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 438 7 1 2 5.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233928 86045 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 438 7 1 2 5.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2308786 86045 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 438 7 1 2 5.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
57758624 106437 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084467 106437 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140096 106437 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11691471 12535 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 398 6 1 1 5.2 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1186783 12535 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 398 6 1 1 5.2 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL478070 12535 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 398 6 1 1 5.2 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCc3ccccc3)(CC1)CC2 10.1021/jm801601v
145951963 162978 0 None -199 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN)=C(/F)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4175500 162978 0 None -199 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN)=C(/F)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
11398062 106435 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 427 6 0 1 6.9 C[N+]1(CC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084464 106435 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 427 6 0 1 6.9 C[N+]1(CC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140094 106435 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 427 6 0 1 6.9 C[N+]1(CC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11692150 12598 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187107 12598 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL490651 12598 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
145950432 162928 0 None -120 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21)=C(\F)CN 10.1021/acsmedchemlett.7b00406
CHEMBL4174727 162928 0 None -120 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 394 6 2 4 3.7 C/C(CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21)=C(\F)CN 10.1021/acsmedchemlett.7b00406
76313456 106482 0 None -1 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
CHEMBL3085066 106482 0 None -1 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
CHEMBL3140216 106482 0 None -1 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1cccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)c1 10.1016/j.bmcl.2007.09.071
66875589 103363 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084662 103363 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11504490 192578 0 None - 0 Human 11.0 pKd = 11 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
CHEMBL521523 192578 0 None - 0 Human 11.0 pKd = 11 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
11504490 192578 0 None - 0 Human 11.0 pKd = 11 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL521523 192578 0 None - 0 Human 11.0 pKd = 11 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
25034186 201415 0 None - 0 Human 10.9 pKd = 10.9 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 722 11 4 8 7.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC4CCCCC4)s3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
CHEMBL540396 201415 0 None - 0 Human 10.9 pKd = 10.9 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 722 11 4 8 7.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC4CCCCC4)s3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
CHEMBL604842 201415 0 None - 0 Human 10.9 pKd = 10.9 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 722 11 4 8 7.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC4CCCCC4)s3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
25195533 78357 2 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2103803 78357 2 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2110584 78357 2 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
25195533 78357 2 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2103803 78357 2 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2110584 78357 2 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
44589580 173124 0 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 635 10 5 7 5.3 C[N+]1(Cc2ccc(O)cc2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC3CCCCC3)s2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL452142 173124 0 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 635 10 5 7 5.3 C[N+]1(Cc2ccc(O)cc2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC3CCCCC3)s2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL553448 173124 0 None - 0 Human 10.7 pKd = 10.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 635 10 5 7 5.3 C[N+]1(Cc2ccc(O)cc2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC3CCCCC3)s2)C1 10.1016/j.bmcl.2008.09.020
11533795 12586 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(F)c3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187076 12586 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(F)c3)(CC1)CC2 10.1021/jm801601v
CHEMBL489212 12586 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(F)c3)(CC1)CC2 10.1021/jm801601v
25034184 188373 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 676 11 4 7 6.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
CHEMBL501803 188373 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 676 11 4 7 6.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
CHEMBL539887 188373 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 676 11 4 7 6.1 Cc1cn2cc(CNC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)OC(C)C)cc3)[n+](Cc3ccc4ccccc4c3)c2s1 10.1021/jm800634k
11442669 74426 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2023760 74426 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2027876 74426 0 None - 0 Human 10.6 pKd = 10.6 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11519069 3908 3 None - 3 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
11519070 3908 3 None - 3 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
4816 3908 3 None - 3 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
7354 3908 3 None - 3 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
CHEMBL1187833 3908 3 None - 3 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
DB09076 3908 3 None - 3 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
11528123 192609 0 None - 0 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 529 8 2 5 4.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL521696 192609 0 None - 0 Human 10.5 pKd = 10.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 529 8 2 5 4.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
42626090 12585 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1187075 12585 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL489211 12585 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
42626094 12593 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3F)(CC1)CC2 10.1021/jm801601v
CHEMBL1187092 12593 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3F)(CC1)CC2 10.1021/jm801601v
CHEMBL490237 12593 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3F)(CC1)CC2 10.1021/jm801601v
11585117 12729 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Br)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187851 12729 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Br)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL523957 12729 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Br)cc3)(CC1)CC2 10.1021/jm801601v
70689729 74450 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 479 10 0 2 6.9 C[N+]1(CCCOCc2ccccc2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2021997 74450 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 479 10 0 2 6.9 C[N+]1(CCCOCc2ccccc2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2028006 74450 0 None - 0 Human 10.4 pKd = 10.4 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 479 10 0 2 6.9 C[N+]1(CCCOCc2ccccc2)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11753447 187327 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 459 7 2 4 4.4 CC(=O)c1cccc(C(=O)NCc2ccc(F)c(-c3cccc(CN4CCN[C@@H](C)C4)c3)c2)c1 10.1021/jm800935u
CHEMBL493265 187327 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 459 7 2 4 4.4 CC(=O)c1cccc(C(=O)NCc2ccc(F)c(-c3cccc(CN4CCN[C@@H](C)C4)c3)c2)c1 10.1021/jm800935u
11365314 187328 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 473 8 2 4 4.8 CCC(=O)c1cccc(C(=O)NCc2ccc(F)c(-c3cccc(CN4CCN[C@@H](C)C4)c3)c2)c1 10.1021/jm800935u
CHEMBL493266 187328 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 473 8 2 4 4.8 CCC(=O)c1cccc(C(=O)NCc2ccc(F)c(-c3cccc(CN4CCN[C@@H](C)C4)c3)c2)c1 10.1021/jm800935u
57758618 106446 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 359 5 0 1 5.3 CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084457 106446 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 359 5 0 1 5.3 CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140108 106446 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 359 5 0 1 5.3 CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
57758626 106462 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 373 6 0 1 5.7 CCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084458 106462 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 373 6 0 1 5.7 CCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140168 106462 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 373 6 0 1 5.7 CCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
57758627 106463 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084459 106463 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140169 106463 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 385 6 0 1 5.7 C[N+]1(CC2CC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44232952 103356 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084650 103356 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
11592005 12715 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1ccc(F)cc1)(c1ccc(F)cc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187807 12715 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1ccc(F)cc1)(c1ccc(F)cc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL522081 12715 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1ccc(F)cc1)(c1ccc(F)cc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
11649606 12721 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 462 8 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Cl)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187835 12721 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 462 8 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Cl)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL523474 12721 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 462 8 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(Cl)cc3)(CC1)CC2 10.1021/jm801601v
11651006 188924 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 573 11 3 6 3.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(CCCO)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL508097 188924 0 None - 0 Human 10.2 pKd = 10.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 573 11 3 6 3.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(CCCO)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
11519318 12712 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(F)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187800 12712 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(F)cc3)(CC1)CC2 10.1021/jm801601v
CHEMBL521781 12712 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 446 8 1 2 5.3 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccc(F)cc3)(CC1)CC2 10.1021/jm801601v
11693689 170904 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 620 10 2 4 5.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(Cc6ccccc6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL445527 170904 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 620 10 2 4 5.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(Cc6ccccc6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL554706 170904 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 620 10 2 4 5.7 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(Cc6ccccc6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
44573747 187693 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 543 9 2 5 3.5 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(C=O)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL495350 187693 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 543 9 2 5 3.5 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCN(C=O)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
70685520 74436 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 443 11 0 1 7.6 CCCCCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2021998 74436 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 443 11 0 1 7.6 CCCCCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2027937 74436 0 None - 0 Human 10.1 pKd = 10.1 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 443 11 0 1 7.6 CCCCCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44233188 103227 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 5 1 2 3.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084419 103227 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 5 1 2 3.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44234688 106453 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 346 3 0 0 5.8 Cc1ccccc1C(=C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3084414 106453 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 346 3 0 0 5.8 Cc1ccccc1C(=C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3140115 106453 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 346 3 0 0 5.8 Cc1ccccc1C(=C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
11223598 106498 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084413 106498 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140264 106498 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
42626019 12533 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL1186756 12533 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL476434 12533 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
25195533 78357 2 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2103803 78357 2 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2110584 78357 2 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11586041 172660 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 572 10 2 4 4.9 CCC[N+]1(C)CCN(Cc2cccc(C(=O)NCc3ccc(F)c(-c4cccc(CN5CCN[C@@H](C)C5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL450060 172660 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 572 10 2 4 4.9 CCC[N+]1(C)CCN(Cc2cccc(C(=O)NCc3ccc(F)c(-c4cccc(CN5CCN[C@@H](C)C5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL540251 172660 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 572 10 2 4 4.9 CCC[N+]1(C)CCN(Cc2cccc(C(=O)NCc3ccc(F)c(-c4cccc(CN5CCN[C@@H](C)C5)c4)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44589581 188764 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 615 12 5 6 4.9 C=CC[N+]1(Cc2cccc(O)c2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC(C)C)cc2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL505751 188764 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 615 12 5 6 4.9 C=CC[N+]1(Cc2cccc(O)c2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC(C)C)cc2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL540145 188764 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 615 12 5 6 4.9 C=CC[N+]1(Cc2cccc(O)c2)CCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)Nc2ccc(C(=O)OC(C)C)cc2)C1 10.1016/j.bmcl.2008.09.020
44589579 189030 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 595 10 5 7 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)s1 10.1016/j.bmcl.2008.09.020
CHEMBL509515 189030 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 595 10 5 7 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)s1 10.1016/j.bmcl.2008.09.020
CHEMBL540148 189030 0 None - 0 Human 10.0 pKd = 10 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 595 10 5 7 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)s1 10.1016/j.bmcl.2008.09.020
44233930 106497 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 363 5 1 1 3.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084409 106497 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 363 5 1 1 3.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140263 106497 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 363 5 1 1 3.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C(N)=O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
42626017 12731 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(Br)c3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187854 12731 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(Br)c3)(CC1)CC2 10.1021/jm801601v
CHEMBL524119 12731 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3cccc(Br)c3)(CC1)CC2 10.1021/jm801601v
25034182 172560 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL448870 172560 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL540359 172560 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
11585987 187694 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 516 8 2 5 4.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCOCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL495358 187694 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 516 8 2 5 4.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCOCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
11607628 188288 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 584 8 2 4 5.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+]6(CCCCC6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL500560 188288 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 584 8 2 4 5.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+]6(CCCCC6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL539886 188288 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 584 8 2 4 5.0 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+]6(CCCCC6)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
25034182 172560 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL448870 172560 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL540359 172560 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
25132856 187192 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 515 8 3 5 3.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
CHEMBL492437 187192 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 515 8 3 5 3.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
25132856 187192 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 515 8 3 5 3.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL492437 187192 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 515 8 3 5 3.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
11556983 187341 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 544 8 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493331 187341 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 544 8 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL538864 187341 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 544 8 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL555476 187341 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 544 8 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CC[N+](C)(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
57758616 106447 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 398 7 0 2 5.6 C[N+]1(CCCC#N)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084463 106447 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 398 7 0 2 5.6 C[N+]1(CCCC#N)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140109 106447 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 398 7 0 2 5.6 C[N+]1(CCCC#N)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
57758629 106469 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 375 6 1 2 4.3 C[N+]1(CCO)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084460 106469 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 375 6 1 2 4.3 C[N+]1(CCO)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140180 106469 0 None - 0 Human 9.8 pKd = 9.8 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 375 6 1 2 4.3 C[N+]1(CCO)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11535362 187594 0 None - 0 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 545 12 2 5 4.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN(C)CCCN(C)C)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL494837 187594 0 None - 0 Human 9.7 pKd = 9.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 545 12 2 5 4.6 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN(C)CCCN(C)C)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
16086059 80746 0 None - 0 Rat 9.7 pKd = 9.7 Functional
Antagonist activity at M3 receptor assessed as inhibition of carbachol-induced contraction of rat tracheaAntagonist activity at M3 receptor assessed as inhibition of carbachol-induced contraction of rat trachea
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL215180 80746 0 None - 0 Rat 9.7 pKd = 9.7 Functional
Antagonist activity at M3 receptor assessed as inhibition of carbachol-induced contraction of rat tracheaAntagonist activity at M3 receptor assessed as inhibition of carbachol-induced contraction of rat trachea
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
11249888 187353 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 442 6 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C#N)c4)ccc3F)c2)CCN1 10.1021/jm800935u
CHEMBL493465 187353 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assayAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
ChEMBL 442 6 2 4 4.1 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C#N)c4)ccc3F)c2)CCN1 10.1021/jm800935u
11642407 12588 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1cccc(F)c1)(c1cccc(F)c1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187079 12588 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1cccc(F)c1)(c1cccc(F)c1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL489625 12588 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 464 8 1 2 5.4 OC(c1cccc(F)c1)(c1cccc(F)c1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
11564285 193131 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 543 8 2 5 4.4 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCCN(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL523044 193131 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 543 8 2 5 4.4 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCCN(C)CC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
44232952 103356 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084650 103356 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11519069 3908 3 None - 3 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
11519070 3908 3 None - 3 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
4816 3908 3 None - 3 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
7354 3908 3 None - 3 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
CHEMBL1187833 3908 3 None - 3 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
DB09076 3908 3 None - 3 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
42625938 12584 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 337 5 2 2 2.9 NCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187073 12584 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 337 5 2 2 2.9 NCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL489032 12584 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 337 5 2 2 2.9 NCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
15951517 12595 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 8 1 2 4.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
CHEMBL1187094 12595 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 8 1 2 4.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
CHEMBL490243 12595 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 8 1 2 4.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
11512119 12722 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 453 8 1 3 5.0 N#Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1187838 12722 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 453 8 1 3 5.0 N#Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL523598 12722 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 453 8 1 3 5.0 N#Cc1ccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
69058946 106448 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084658 106448 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140110 106448 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
69058946 106448 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084658 106448 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3140110 106448 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
42625944 12573 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 426 8 1 1 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1186964 12573 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 426 8 1 1 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL484475 12573 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 426 8 1 1 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCc3ccccc3)(CC1)CC2 10.1021/jm801601v
16041939 12596 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 423 8 0 2 5.3 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
CHEMBL1187095 12596 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 423 8 0 2 5.3 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
CHEMBL490244 12596 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 423 8 0 2 5.3 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)C2 10.1021/jm801601v
57758617 106434 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 389 7 0 2 4.9 COCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084462 106434 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 389 7 0 2 4.9 COCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140093 106434 0 None - 0 Human 9.3 pKd = 9.3 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 389 7 0 2 4.9 COCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11636578 193053 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 514 8 2 4 5.2 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCCCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL522495 193053 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 514 8 2 4 5.2 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN5CCCCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
44589582 171617 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 12 4 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](CC3CC3)(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL446587 171617 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 12 4 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](CC3CC3)(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL550885 171617 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 12 4 5 4.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](CC3CC3)(CC3CC3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589576 189032 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 6 5 3.9 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL509520 189032 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 6 5 3.9 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555706 189032 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 6 5 3.9 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
57758613 106473 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 433 10 0 3 4.9 COCCOCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084468 106473 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 433 10 0 3 4.9 COCCOCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140184 106473 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 433 10 0 3 4.9 COCCOCC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
11705920 12717 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 7 1 2 5.0 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187810 12717 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 7 1 2 5.0 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL522418 12717 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 414 7 1 2 5.0 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
11633226 106501 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 344 3 0 2 5.6 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084418 106501 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 344 3 0 2 5.6 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140267 106501 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 344 3 0 2 5.6 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
11223598 106498 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084413 106498 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140264 106498 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contractionAntagonist activity at human muscarinic M3 receptor in human bronchus assessed as potency against carbachol-induced contraction
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
11691950 12730 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187853 12730 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL524097 12730 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contractionAntagonist activity at human muscarinic M3 receptor assessed as inhibition of carbachol-induced bronchus contraction
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
57758623 106471 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 371 6 0 1 5.5 C=CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084461 106471 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 371 6 0 1 5.5 C=CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140182 106471 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to controlAntagonist potency at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis relative to control
ChEMBL 371 6 0 1 5.5 C=CC[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44234690 106500 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 4 1 1 4.7 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084417 106500 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 4 1 1 4.7 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140266 106500 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 4 1 1 4.7 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44232949 106499 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 362 4 1 3 4.8 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084415 106499 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 362 4 1 3 4.8 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140265 106499 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 362 4 1 3 4.8 C[N+]1(C)[C@H]2CCC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
11635210 12704 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 458 9 1 3 5.1 COc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL1187765 12704 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 458 9 1 3 5.1 COc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL519652 12704 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 458 9 1 3 5.1 COc1cccc(COCC[N+]23CCC(C(O)(c4ccccc4)c4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
44589578 173146 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1nc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)no1 10.1016/j.bmcl.2008.09.020
CHEMBL452193 173146 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1nc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)no1 10.1016/j.bmcl.2008.09.020
CHEMBL540401 173146 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1nc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)no1 10.1016/j.bmcl.2008.09.020
44589577 188944 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1noc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)n1 10.1016/j.bmcl.2008.09.020
CHEMBL508343 188944 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1noc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)n1 10.1016/j.bmcl.2008.09.020
CHEMBL540146 188944 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 585 9 5 7 4.1 Cc1noc(-c2ccc(NC(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H]3CCC[N+](C)(Cc4ccc(O)cc4)C3)cc2)n1 10.1016/j.bmcl.2008.09.020
44232702 106476 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3084401 106476 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3140203 106476 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
11692150 12598 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187107 12598 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL490651 12598 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 9 1 2 5.8 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
25034182 172560 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL448870 172560 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL540359 172560 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
76327869 103224 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 333 4 1 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084396 103224 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 333 4 1 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
66875589 103363 0 None - 1 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084662 103363 0 None - 1 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11235700 106440 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084410 106440 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140099 106440 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccs1)c1cccs1)C2 10.1021/jm900736e
66875589 103363 0 None - 1 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084662 103363 0 None - 1 Human 8.6 pKd = 8.6 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
44233192 106455 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084643 106455 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3140141 106455 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
42626088 12592 0 None - 1 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
CHEMBL1187091 12592 0 None - 1 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
CHEMBL490236 12592 0 None - 1 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 506 8 1 2 5.9 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3Br)(CC1)CC2 10.1021/jm801601v
42626013 12594 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 437 8 0 2 5.7 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187093 12594 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 437 8 0 2 5.7 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL490242 12594 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 437 8 0 2 5.7 N#CC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2 10.1021/jm801601v
11722039 187340 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 530 8 3 4 3.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C[N+]5(C)CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493330 187340 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 530 8 3 4 3.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C[N+]5(C)CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL558605 187340 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 530 8 3 4 3.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(C[N+]5(C)CCNCC5)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
11650778 187448 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 474 8 2 4 4.3 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN(C)C)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL494022 187448 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR based single concentration kinetic assay
ChEMBL 474 8 2 4 4.3 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CN(C)C)c4)ccc3F)c2)CCN1 10.1016/j.bmcl.2009.01.098
16042745 185277 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 551 8 4 5 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+]3(CCCCCC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL485932 185277 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 551 8 4 5 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+]3(CCCCCC3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL538360 185277 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 551 8 4 5 4.4 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+]3(CCCCCC3)C2)cc1 10.1016/j.bmcl.2008.09.020
44233190 103375 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084679 103375 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233192 106455 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084643 106455 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140141 106455 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233190 103375 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084679 103375 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assayAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by measuring ratio of acetylcholine EC50 in presence and absence of compound by FLIPR assay
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
42626092 12603 0 None - 1 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187132 12603 0 None - 1 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL491246 12603 0 None - 1 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic based-FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
66604762 106483 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 318 3 0 0 5.1 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084398 106483 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 318 3 0 0 5.1 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3140217 106483 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 318 3 0 0 5.1 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44232700 106484 0 None - 1 Human 8.3 pKd = 8.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3084399 106484 0 None - 1 Human 8.3 pKd = 8.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3140218 106484 0 None - 1 Human 8.3 pKd = 8.3 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
16065402 67898 0 None - 0 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 428 9 1 3 4.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910848 67898 0 None - 0 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 428 9 1 3 4.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2)C1 10.1021/jm200884j
367 3795 12 None -3 8 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
5487427 3795 12 None -3 8 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
8592 3795 12 None -3 8 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL1900528 3795 12 None -3 8 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL3305968 3795 12 None -3 8 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL4650755 3795 12 None -3 8 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
DB01409 3795 12 None -3 8 Human 10.3 pKi = 10.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
54757541 67902 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2O)C1 10.1021/jm200884j
CHEMBL1910852 67902 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2O)C1 10.1021/jm200884j
54757856 67907 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 10 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(OCc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910857 67907 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 10 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(OCc2cccc(O)c2)C1 10.1021/jm200884j
25897919 55622 14 None -1 5 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
657309 55622 14 None -1 5 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
CHEMBL1464005 55622 14 None -1 5 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
CHEMBL1621597 55622 14 None -1 5 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
16065403 67906 23 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910856 67906 23 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1 10.1021/jm200884j
16034837 67901 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910851 67901 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
16065543 67912 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 478 9 2 4 5.1 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)cc(Cl)c2)C1 10.1021/jm200884j
CHEMBL1910862 67912 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 478 9 2 4 5.1 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)cc(Cl)c2)C1 10.1021/jm200884j
16065135 67896 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910846 67896 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2)C1 10.1021/jm200884j
16065407 67915 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2F)C1 10.1021/jm200884j
CHEMBL1910865 67915 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2F)C1 10.1021/jm200884j
16065268 67899 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 456 9 1 3 5.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2ccccc2)CC1 10.1021/jm200884j
CHEMBL1910849 67899 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 456 9 1 3 5.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2ccccc2)CC1 10.1021/jm200884j
16065137 67900 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910850 67900 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
54757544 67910 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 476 9 2 4 5.0 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cc(O)cc(F)c2)C1 10.1021/jm200884j
CHEMBL1910860 67910 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 476 9 2 4 5.0 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cc(O)cc(F)c2)C1 10.1021/jm200884j
16065405 67913 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)cc(F)c2)C1 10.1021/jm200884j
CHEMBL1910863 67913 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)cc(F)c2)C1 10.1021/jm200884j
16065541 67916 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)ccc2F)C1 10.1021/jm200884j
CHEMBL1910866 67916 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)ccc2F)C1 10.1021/jm200884j
16065406 67908 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 470 9 2 4 5.0 NC(=O)C(CCC1(N2CC(Oc3cccc(O)c3)C2)CCCC1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
CHEMBL1910858 67908 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 470 9 2 4 5.0 NC(=O)C(CCC1(N2CC(Oc3cccc(O)c3)C2)CCCC1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
54757543 67903 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccc(O)cc2)C1 10.1021/jm200884j
CHEMBL1910853 67903 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccc(O)cc2)C1 10.1021/jm200884j
16065136 67897 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910847 67897 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2ccccc2)C1 10.1021/jm200884j
16065404 67911 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 478 9 2 4 5.1 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccc(Cl)c(O)c2)C1 10.1021/jm200884j
CHEMBL1910861 67911 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 478 9 2 4 5.1 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccc(Cl)c(O)c2)C1 10.1021/jm200884j
126534204 138407 0 None - 0 Human 6.0 pKi = 6.0 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 504 7 1 7 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1cc[nH]c(=O)c1 10.1016/j.bmc.2016.02.031
CHEMBL3774411 138407 0 None - 0 Human 6.0 pKi = 6.0 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 504 7 1 7 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1cc[nH]c(=O)c1 10.1016/j.bmc.2016.02.031
54757653 67905 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2O)C1 10.1021/jm200884j
CHEMBL1910855 67905 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2O)C1 10.1021/jm200884j
121304590 145333 0 None - 0 Human 5.9 pKi = 5.9 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3913607 145333 0 None - 0 Human 5.9 pKi = 5.9 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
121304477 152147 0 None - 0 Human 5.9 pKi = 5.9 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 487 7 0 6 5.6 Cc1ncccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3968272 152147 0 None - 0 Human 5.9 pKi = 5.9 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 487 7 0 6 5.6 Cc1ncccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
126534771 138568 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 424 7 0 8 3.5 Cc1ncoc1-c1nnc(SCCCN2CC3CCN(c4ccccc4)C3C2)n1C 10.1016/j.bmc.2016.02.031
CHEMBL3775589 138568 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 424 7 0 8 3.5 Cc1ncoc1-c1nnc(SCCCN2CC3CCN(c4ccccc4)C3C2)n1C 10.1016/j.bmc.2016.02.031
126533969 138443 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 427 7 0 7 3.4 Cn1c(SCCCN2CC3CCN(c4ccccc4)C3C2)nnc1C1CCOCC1 10.1016/j.bmc.2016.02.031
CHEMBL3774649 138443 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 427 7 0 7 3.4 Cn1c(SCCCN2CC3CCN(c4ccccc4)C3C2)nnc1C1CCOCC1 10.1016/j.bmc.2016.02.031
121304609 152937 0 None - 0 Human 5.8 pKi = 5.8 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(F)cc3C(F)(F)F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3975147 152937 0 None - 0 Human 5.8 pKi = 5.8 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(F)cc3C(F)(F)F)C2)n1C 10.1021/acs.jmedchem.6b00972
121304654 148853 0 None - 0 Human 6.7 pKi = 6.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 530 8 1 7 4.7 Cc1nc(C(N)=O)ccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3941520 148853 0 None - 0 Human 6.7 pKi = 6.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 530 8 1 7 4.7 Cc1nc(C(N)=O)ccc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
121304538 149981 0 None - 0 Human 6.7 pKi = 6.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 516 8 1 7 4.4 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)nc1 10.1021/acs.jmedchem.6b00972
CHEMBL3950254 149981 0 None - 0 Human 6.7 pKi = 6.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 516 8 1 7 4.4 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)nc1 10.1021/acs.jmedchem.6b00972
54757542 67909 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 492 9 2 4 5.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccc(Cl)c(O)c2)C1 10.1021/jm200884j
CHEMBL1910859 67909 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 492 9 2 4 5.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccc(Cl)c(O)c2)C1 10.1021/jm200884j
16065269 67904 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 472 9 2 4 5.3 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2cccc(O)c2)CC1 10.1021/jm200884j
CHEMBL1910854 67904 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 472 9 2 4 5.3 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2cccc(O)c2)CC1 10.1021/jm200884j
54757332 67895 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 414 9 1 3 4.4 NC(=O)C(CCCN1CC[C@H](Oc2ccccc2)C1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
CHEMBL1910845 67895 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 414 9 1 3 4.4 NC(=O)C(CCCN1CC[C@H](Oc2ccccc2)C1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
121304458 153965 0 None - 0 Human 5.7 pKi = 5.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 409 7 0 7 4.1 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccccc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3983937 153965 0 None - 0 Human 5.7 pKi = 5.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 409 7 0 7 4.1 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccccc3)C2)n1C 10.1021/acs.jmedchem.6b00972
121304867 154175 0 None - 0 Human 5.7 pKi = 5.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@H]3c3ccc(F)cc3C(F)(F)F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3985877 154175 0 None - 0 Human 5.7 pKi = 5.7 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@H]3c3ccc(F)cc3C(F)(F)F)C2)n1C 10.1021/acs.jmedchem.6b00972
126534291 138516 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 488 7 0 7 4.6 Cn1c(SCCCN2CC3CCN(c4ccccc4C(F)(F)F)C3C2)nnc1-c1cccnc1 10.1016/j.bmc.2016.02.031
CHEMBL3775197 138516 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 488 7 0 7 4.6 Cn1c(SCCCN2CC3CCN(c4ccccc4C(F)(F)F)C3C2)nnc1-c1cccnc1 10.1016/j.bmc.2016.02.031
121304598 145221 0 None - 0 Human 6.6 pKi = 6.6 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 535 8 1 6 5.4 CC(=O)NC1CCC(c2nnc(SCCCN3CC[C@]4(C[C@@H]4c4ccc(C(F)(F)F)cc4)C3)n2C)CC1 10.1021/acs.jmedchem.6b00972
CHEMBL3912801 145221 0 None - 0 Human 6.6 pKi = 6.6 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 535 8 1 6 5.4 CC(=O)NC1CCC(c2nnc(SCCCN3CC[C@]4(C[C@@H]4c4ccc(C(F)(F)F)cc4)C3)n2C)CC1 10.1021/acs.jmedchem.6b00972
126534373 138521 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 510 7 0 8 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4F)C3C2)n1C 10.1016/j.bmc.2016.02.031
CHEMBL3775226 138521 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 510 7 0 8 4.6 Cc1ncoc1-c1nnc(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4F)C3C2)n1C 10.1016/j.bmc.2016.02.031
121304464 144319 0 None - 0 Human 6.6 pKi = 6.6 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 480 7 0 8 4.7 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1csnn1 10.1021/acs.jmedchem.6b00972
CHEMBL3905582 144319 0 None - 0 Human 6.6 pKi = 6.6 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 480 7 0 8 4.7 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1csnn1 10.1021/acs.jmedchem.6b00972
121304485 148151 0 None - 0 Human 6.6 pKi = 6.6 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3935692 148151 0 None - 0 Human 6.6 pKi = 6.6 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 477 7 0 7 5.2 Cc1ncoc1-c1nnc(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)n1C 10.1021/acs.jmedchem.6b00972
10125445 75999 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at muscarinic M3 receptorAntagonist activity at muscarinic M3 receptor
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1021/jm800582j
CHEMBL205654 75999 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at muscarinic M3 receptorAntagonist activity at muscarinic M3 receptor
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1021/jm800582j
121304452 148894 0 None - 0 Human 6.5 pKi = 6.5 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 539 8 0 7 6.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(-c2ncco2)cc1 10.1021/acs.jmedchem.6b00972
CHEMBL3941818 148894 0 None - 0 Human 6.5 pKi = 6.5 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 539 8 0 7 6.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(-c2ncco2)cc1 10.1021/acs.jmedchem.6b00972
121304574 143008 0 None - 0 Human 6.5 pKi = 6.5 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 503 7 0 7 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccn(C)c(=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL3894853 143008 0 None - 0 Human 6.5 pKi = 6.5 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 503 7 0 7 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccn(C)c(=O)c1 10.1021/acs.jmedchem.6b00972
121304441 152360 0 None - 0 Human 6.4 pKi = 6.4 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL3970323 152360 0 None - 0 Human 6.4 pKi = 6.4 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
121304408 143529 0 None - 0 Human 6.4 pKi = 6.4 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)cc1 10.1021/acs.jmedchem.6b00972
CHEMBL3899125 143529 0 None - 0 Human 6.4 pKi = 6.4 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1ccc(C(N)=O)cc1 10.1021/acs.jmedchem.6b00972
121304649 150621 0 None - 0 Human 6.4 pKi = 6.4 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3955505 150621 0 None - 0 Human 6.4 pKi = 6.4 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
126535075 138454 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 518 7 0 8 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1ccc(=O)n(C)c1 10.1016/j.bmc.2016.02.031
CHEMBL3774769 138454 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assayAntagonist activity at recombinant human muscarinic M3 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition measured after 1 hr by fluo-4 AM dye-based FLIPR assay
ChEMBL 518 7 0 8 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1ccc(=O)n(C)c1 10.1016/j.bmc.2016.02.031
121304424 143819 0 None - 0 Human 6.3 pKi = 6.3 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
CHEMBL3901587 143819 0 None - 0 Human 6.3 pKi = 6.3 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 495 7 0 7 5.3 Cc1ncoc1-c1nnc(SCCCN2CC[C@@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/acs.jmedchem.6b00972
134150754 151705 0 None - 0 Human 6.2 pKi = 6.2 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 489 7 0 6 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1=CCC(=O)N=C1 10.1021/acs.jmedchem.6b00972
CHEMBL3964512 151705 0 None - 0 Human 6.2 pKi = 6.2 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 489 7 0 6 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1=CCC(=O)N=C1 10.1021/acs.jmedchem.6b00972
134134147 143349 0 None - 0 Human 6.2 pKi = 6.2 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 489 7 0 6 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1=CC=NC(=O)C1 10.1021/acs.jmedchem.6b00972
CHEMBL3897772 143349 0 None - 0 Human 6.2 pKi = 6.2 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 489 7 0 6 4.6 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1=CC=NC(=O)C1 10.1021/acs.jmedchem.6b00972
134150637 151541 0 None - 0 Human 6.2 pKi = 6.2 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 522 7 1 6 4.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCN(C(N)=O)CC1 10.1021/acs.jmedchem.6b00972
CHEMBL3963243 151541 0 None - 0 Human 6.2 pKi = 6.2 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 522 7 1 6 4.5 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCN(C(N)=O)CC1 10.1021/acs.jmedchem.6b00972
54757766 67914 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 512 9 2 4 5.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)c(Cl)cc2Cl)C1 10.1021/jm200884j
CHEMBL1910864 67914 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetryAntagonist activity at human recombinant M3 receptor expressed in CHO-K1 cells assessed as inhibition of carbamoyl choline-induced calcium currents after 4 hrs by fluorimetry
ChEMBL 512 9 2 4 5.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cc(O)c(Cl)cc2Cl)C1 10.1021/jm200884j
483747 105382 3 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonistic activity against muscarinic M3 receptorAntagonistic activity against muscarinic M3 receptor
ChEMBL 503 4 0 5 4.9 Cc1ncnc(C)c1C(=O)N1CCC(C)(N2CCN([C@@H](C)c3ccc(C(F)(F)F)cc3)[C@@H](C)C2)CC1 10.1021/jm0304515
CHEMBL311795 105382 3 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonistic activity against muscarinic M3 receptorAntagonistic activity against muscarinic M3 receptor
ChEMBL 503 4 0 5 4.9 Cc1ncnc(C)c1C(=O)N1CCC(C)(N2CCN([C@@H](C)c3ccc(C(F)(F)F)cc3)[C@@H](C)C2)CC1 10.1021/jm0304515
121304500 149730 0 None - 0 Human 6.1 pKi = 6.1 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 480 7 0 6 5.1 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCOCC1 10.1021/acs.jmedchem.6b00972
CHEMBL3948167 149730 0 None - 0 Human 6.1 pKi = 6.1 Functional
Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assayActivity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
ChEMBL 480 7 0 6 5.1 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1C1CCOCC1 10.1021/acs.jmedchem.6b00972
3009352 96610 1 None - 0 Human 5.0 pKi = 5.0 Functional
Antagonistic activity against muscarinic M3 receptorAntagonistic activity against muscarinic M3 receptor
ChEMBL 517 5 0 5 5.3 CC[C@@H](c1ccc(C(F)(F)F)cc1)N1CCN(C2(C)CCN(C(=O)c3c(C)ncnc3C)CC2)C[C@@H]1C 10.1021/jm0304515
CHEMBL263555 96610 1 None - 0 Human 5.0 pKi = 5.0 Functional
Antagonistic activity against muscarinic M3 receptorAntagonistic activity against muscarinic M3 receptor
ChEMBL 517 5 0 5 5.3 CC[C@@H](c1ccc(C(F)(F)F)cc1)N1CCN(C2(C)CCN(C(=O)c3c(C)ncnc3C)CC2)C[C@@H]1C 10.1021/jm0304515
316 2816 19 None 2 8 Rat 8.0 pEC50 = 8.0 Functional
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
317 2816 19 None 2 8 Rat 8.0 pEC50 = 8.0 Functional
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
71183 2816 19 None 2 8 Rat 8.0 pEC50 = 8.0 Functional
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL3140030 2816 19 None 2 8 Rat 8.0 pEC50 = 8.0 Functional
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL376897 2816 19 None 2 8 Rat 8.0 pEC50 = 8.0 Functional
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
DB00462 2816 19 None 2 8 Rat 8.0 pEC50 = 8.0 Functional
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
1979 77297 70 None -1 7 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
CHEMBL20835 77297 70 None -1 7 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
187 255 39 None -1 8 Human 8.2 pEC50 = 8.2 Functional
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
294 255 39 None -1 8 Human 8.2 pEC50 = 8.2 Functional
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
65 255 39 None -1 8 Human 8.2 pEC50 = 8.2 Functional
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
8593 255 39 None -1 8 Human 8.2 pEC50 = 8.2 Functional
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
CHEMBL667 255 39 None -1 8 Human 8.2 pEC50 = 8.2 Functional
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
DB03128 255 39 None -1 8 Human 8.2 pEC50 = 8.2 Functional
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
Drug Central 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
1726 2480 13 None -5 8 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
1993 2480 13 None -5 8 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
7438 2480 13 None -5 8 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
CHEMBL978 2480 13 None -5 8 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
DB06709 2480 13 None -5 8 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C None
2166 3101 49 None -1 10 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
305 3101 49 None -1 10 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
5910 3101 49 None -1 10 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
CHEMBL550 3101 49 None -1 10 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
DB01085 3101 49 None -1 10 Human 8.2 pEC50 = 8.2 Functional
calcium response in CHO cellscalcium response in CHO cells
Drug Central 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C None
123603 880 29 None -1 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
2684 880 29 None -1 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
584 880 29 None -1 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
9658 880 29 None -1 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
CHEMBL168815 880 29 None -1 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 None
5831 215938 0 None -1 5 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
3008304 3992 52 None -1 4 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 19438238
7632 3992 52 None -1 4 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 19438238
CHEMBL523685 3992 52 None -1 4 Human 5.2 pEC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 19438238
1726 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
1726 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
1993 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
1993 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
7438 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
7438 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
CHEMBL978 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
CHEMBL978 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
DB06709 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
DB06709 2480 13 None -5 8 Rat 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 9622546
288 251 0 None -3 5 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@H]1C[NH+]2CCC1CC2 8968358
6979053 251 0 None -3 5 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@H]1C[NH+]2CCC1CC2 8968358
286 252 0 None -3 5 Human 5.7 pEC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@@H]1C[NH+]2CCC1CC2 8968358
6954180 252 0 None -3 5 Human 5.7 pEC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 170 1 1 2 -0.8 CC(=O)O[C@@H]1C[NH+]2CCC1CC2 8968358
20824 217672 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 378 5 3 5 0.5 CC1(C)S[C@@H]2[C@H](NC(=O)C(C(O)=O)C3=CC=CC=C3)C(=O)N2[C@H]1C(O)=O None
18381 217679 0 None -1 4 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 469 4 2 6 3.2 CC1=C(C(=O)N[C@H]2[C@H]3SC(C)(C)[C@@H](N3C2=O)C(O)=O)C(=NO1)C1=C(Cl)C=CC=C1Cl None
11693 1814 16 None 1 7 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
11693 1814 16 None 1 7 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
3494 1814 16 None 1 7 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
3494 1814 16 None 1 7 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
4302 1814 16 None 1 7 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
4302 1814 16 None 1 7 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
7459 1814 16 None 1 7 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
7459 1814 16 None 1 7 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
CHEMBL1201335 1814 16 None 1 7 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
CHEMBL1201335 1814 16 None 1 7 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
DB00986 1814 16 None 1 7 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 21036043
DB00986 1814 16 None 1 7 Human 9.7 pIC50 = 9.7 Functional
Assay uses glycopyrronium bromideAssay uses glycopyrronium bromide
Guide to Pharmacology 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 22854200
154059 3610 51 None -1 3 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
2457 3610 51 None -1 3 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
7483 3610 51 None -1 3 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
CHEMBL1734 3610 51 None -1 3 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
DB01591 3610 51 None -1 3 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 21524581
6433090 217716 0 None -1 2 Human 8.0 pKb = 8.0 Functional
NoneNone
Drug Central 319 6 1 3 3.1 CC1=NC=CN1CCC(C(N)=O)(C1=CC=CC=C1)C1=CC=CC=C1 None


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
367 3795 12 None 2 8 Human 9.4 pAC50 = 9.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3795 12 None 2 8 Human 9.4 pAC50 = 9.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3795 12 None 2 8 Human 9.4 pAC50 = 9.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3795 12 None 2 8 Human 9.4 pAC50 = 9.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3795 12 None 2 8 Human 9.4 pAC50 = 9.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3795 12 None 2 8 Human 9.4 pAC50 = 9.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3795 12 None 2 8 Human 9.4 pAC50 = 9.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 55622 14 None 1 8 Human 8.8 pAC50 = 8.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 55622 14 None 1 8 Human 8.8 pAC50 = 8.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
CHEMBL1464005 55622 14 None 1 8 Human 8.8 pAC50 = 8.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 55622 14 None 1 8 Human 8.8 pAC50 = 8.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1814 16 None -1 5 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1814 16 None -1 5 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1814 16 None -1 5 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1814 16 None -1 5 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1814 16 None -1 5 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1814 16 None -1 5 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 949 13 None -6 3 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
351 949 13 None -6 3 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
366 949 13 None -6 3 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
676 949 13 None -6 3 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 949 13 None -6 3 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 949 13 None -6 3 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3536 38 None 1 6 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3536 38 None 1 6 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3536 38 None 1 6 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3536 38 None 1 6 Human 8.7 pAC50 = 8.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 504 81 None -19 42 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
249 504 81 None -19 42 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 504 81 None -19 42 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 504 81 None -19 42 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 504 81 None -19 42 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4076 53 None - 8 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4076 53 None - 8 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4076 53 None - 8 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4076 53 None - 8 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4076 53 None - 8 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 136943 32 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 136943 32 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 136943 32 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3073 30 None - 6 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3073 30 None - 6 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3073 30 None - 6 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3073 30 None - 6 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3073 30 None - 6 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 15544 49 None -1 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 15544 49 None -1 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 15544 49 None -1 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 111554 48 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 111554 48 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 205504 62 None -12 26 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 205504 62 None -12 26 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 205504 62 None -12 26 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 57377 25 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 57377 25 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 124064 23 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 124064 23 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1402 35 None -1 15 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1402 35 None -1 15 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1402 35 None -1 15 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1402 35 None -1 15 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1402 35 None -1 15 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 946 33 None -56 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 946 33 None -56 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
671 946 33 None -56 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 946 33 None -56 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 946 33 None -56 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3160 33 None -10 29 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3160 33 None -10 29 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3160 33 None -10 29 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3160 33 None -10 29 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3160 33 None -10 29 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 593 53 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
312 593 53 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 593 53 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 593 53 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 593 53 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3151 58 None -21 32 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3151 58 None -21 32 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3151 58 None -21 32 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3151 58 None -21 32 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3151 58 None -21 32 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 99295 70 None -134 18 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 99295 70 None -134 18 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14461 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14461 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14461 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14461 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14461 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14461 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 31191 105 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 31191 105 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 62455 57 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 62455 57 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 62455 57 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 78144 38 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 78144 38 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 207218 40 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 207218 40 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 206211 23 None -2 9 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 206211 23 None -2 9 Human 6.9 pAC50 = 6.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 7853 104 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 7853 104 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 7853 104 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4369 111 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4369 111 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2333 53 None -19 45 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2333 53 None -19 45 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2333 53 None -19 45 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2333 53 None -19 45 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2333 53 None -19 45 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 78370 31 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 78370 31 None - 0 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 935 74 None - 1 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 935 74 None - 1 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
647 935 74 None - 1 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 935 74 None - 1 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 935 74 None - 1 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 9393 59 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 9393 59 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 82379 49 None -14 24 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 82379 49 None -14 24 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 98045 57 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 98045 57 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 916 68 None -18 73 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
621 916 68 None -18 73 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
83 916 68 None -18 73 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 916 68 None -18 73 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 916 68 None -18 73 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 15262 12 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 15262 12 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 196463 85 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 196463 85 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 194703 86 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 194703 86 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 951 62 None -1 29 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 951 62 None -1 29 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
701 951 62 None -1 29 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 951 62 None -1 29 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 951 62 None -1 29 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1617 26 None - 12 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1617 26 None - 12 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1617 26 None - 12 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1617 26 None - 12 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1617 26 None - 12 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 35031 9 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 35031 9 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 35031 9 None - 0 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4269 49 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4269 49 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4269 49 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 178768 94 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 178768 94 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 11228 36 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 11228 36 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 202110 58 None - 5 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 202110 58 None - 5 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1312 44 None 2 9 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1312 44 None 2 9 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1312 44 None 2 9 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1312 44 None 2 9 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1312 44 None 2 9 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1312 44 None 2 9 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2169 50 None -57 21 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2169 50 None -57 21 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2169 50 None -57 21 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2169 50 None -57 21 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2169 50 None -57 21 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14438 35 None - 0 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14438 35 None - 0 Human 6.8 pAC50 = 6.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1420 83 None -5 13 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1420 83 None -5 13 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1420 83 None -5 13 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1420 83 None -5 13 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1420 83 None -5 13 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1420 83 None -5 13 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 205948 74 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 205948 74 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2327 117 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2327 117 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2327 117 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2327 117 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2327 117 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 96519 28 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 96519 28 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 55390 17 None - 0 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 55390 17 None - 0 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3813 64 None -1 10 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3813 64 None -1 10 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3813 64 None -1 10 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3813 64 None -1 10 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3813 64 None -1 10 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14467 8 None - 0 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14467 8 None - 0 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2515 43 None -22 58 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2515 43 None -22 58 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2515 43 None -22 58 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2515 43 None -22 58 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2515 43 None -22 58 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3109 46 None -7 13 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3109 46 None -7 13 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3109 46 None -7 13 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3109 46 None -7 13 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3109 46 None -7 13 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 6 None -4 5 Human 8.6 pAC50 = 8.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 6 None -4 5 Human 8.6 pAC50 = 8.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 6 None -4 5 Human 8.6 pAC50 = 8.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 6 None -4 5 Human 8.6 pAC50 = 8.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 6 None -4 5 Human 8.6 pAC50 = 8.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 6 None -4 5 Human 8.6 pAC50 = 8.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 102703 47 None - 6 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 102703 47 None - 6 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1213 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
2725 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
33036 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
4411 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
616 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
6976 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
716121 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
90475904 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1201353 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1554789 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL505 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB01114 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB13679 915 51 None -79 21 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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(CCC(c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
47472 19405 57 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 19405 57 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 57376 54 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 57376 54 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 194661 40 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 194661 40 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3563 83 None -239 49 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3563 83 None -239 49 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3563 83 None -239 49 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3563 83 None -239 49 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3563 83 None -239 49 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 27956 53 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 27956 53 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 93905 123 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 93905 123 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 203556 29 None -1 12 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 203556 29 None -1 12 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 120222 49 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 120222 49 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14388 80 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14388 80 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 594 24 None -1 20 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
333 594 24 None -1 20 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 594 24 None -1 20 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 594 24 None -1 20 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 594 24 None -1 20 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 594 24 None -1 20 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
180 400 56 None -23 40 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
200 400 56 None -23 40 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 400 56 None -23 40 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 400 56 None -23 40 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 400 56 None -23 40 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 102831 97 None -6 25 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 102831 97 None -6 25 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 154832 29 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 154832 29 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2742 19 None - 19 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2742 19 None - 19 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2742 19 None - 19 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 12964 54 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 12964 54 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 35300 18 None - 10 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 35300 18 None - 10 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 35300 18 None - 10 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 78111 0 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 204382 53 None -5 23 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 204382 53 None -5 23 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 204382 53 None -5 23 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
CHEMBL5292015 194514 0 None - 0 Human 8.5 pAC50 = 8.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
191 402 98 None -37 29 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
201 402 98 None -37 29 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 402 98 None -37 29 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 402 98 None -37 29 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 402 98 None -37 29 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14460 19 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14460 19 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14460 19 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14460 19 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3161 51 None -1 30 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3161 51 None -1 30 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3161 51 None -1 30 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3161 51 None -1 30 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3161 51 None -1 30 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4122 61 None -144 54 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4122 61 None -144 54 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4122 61 None -144 54 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4122 61 None -144 54 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 4122 61 None -144 54 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 203569 41 None -1 8 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 203569 41 None -1 8 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 29245 76 None - 5 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 29245 76 None - 5 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 29245 76 None - 5 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 12498 6 None - 0 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 12498 6 None - 0 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 16617 50 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 16617 50 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 16617 50 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2893 112 None -27 66 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2893 112 None -27 66 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2893 112 None -27 66 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2893 112 None -27 66 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3839 95 None -2 10 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3839 95 None -2 10 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3839 95 None -2 10 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3839 95 None -2 10 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3839 95 None -2 10 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3839 95 None -2 10 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 56237 27 None -104 20 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 56237 27 None -104 20 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 9125 37 None - 0 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 9125 37 None - 0 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 23149 60 None -1 5 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 23149 60 None -1 5 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14466 50 None - 5 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14466 50 None - 5 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 41691 15 None -1 9 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 41691 15 None -1 9 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 11816 22 None -1 12 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 11816 22 None -1 12 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 11816 22 None -1 12 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 11816 22 None -1 12 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 186896 64 None -5 25 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 186896 64 None -5 25 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 186896 64 None -5 25 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 206372 53 None -4 16 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 206372 53 None -4 16 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14443 26 None - 0 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14443 26 None - 0 Human 8.3 pAC50 = 8.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 955 93 None -10 92 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
38 955 93 None -10 92 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
722 955 93 None -10 92 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 955 93 None -10 92 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 955 93 None -10 92 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 196412 120 None - 0 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 196412 120 None - 0 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3840 54 None - 6 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3840 54 None - 6 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3840 54 None - 6 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3840 54 None - 6 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3840 54 None - 6 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2846 38 None -4 30 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2846 38 None -4 30 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2846 38 None -4 30 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2846 38 None -4 30 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2846 38 None -4 30 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14379 30 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 14379 30 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 18953 99 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 18953 99 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 99285 28 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 99285 28 None - 0 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1645 75 None -30 32 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1645 75 None -30 32 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1645 75 None -30 32 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1645 75 None -30 32 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1645 75 None -30 32 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 89565 85 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 89565 85 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 67579 43 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 67579 43 None - 2 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3536 38 None 1 6 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3536 38 None 1 6 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3536 38 None 1 6 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3536 38 None 1 6 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 17960 31 None - 6 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 17960 31 None - 6 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 37378 106 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 37378 106 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1377 114 None -9 15 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1377 114 None -9 15 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1377 114 None -9 15 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1377 114 None -9 15 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1377 114 None -9 15 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3831 58 None -93 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3831 58 None -93 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3831 58 None -93 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3831 58 None -93 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3831 58 None -93 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3831 58 None -93 30 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 17926 26 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 17926 26 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 205248 82 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 205248 82 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 205248 82 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 205248 82 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 205248 82 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 205248 82 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 205248 82 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2000 54 None -2 27 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2000 54 None -2 27 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2000 54 None -2 27 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2000 54 None -2 27 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 2000 54 None -2 27 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 67372 13 None 1 5 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 67372 13 None 1 5 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 67372 13 None 1 5 Human 8.1 pAC50 = 8.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 178204 69 None - 3 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 178204 69 None - 3 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1651 49 None - 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1651 49 None - 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1651 49 None - 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1651 49 None - 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1651 49 None - 33 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 5686 50 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 5686 50 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 12582 15 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 12582 15 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3776 58 None -8 56 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3776 58 None -8 56 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3776 58 None -8 56 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3776 58 None -8 56 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3776 58 None -8 56 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 67541 104 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 67541 104 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3232 77 None -81 63 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3232 77 None -81 63 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3232 77 None -81 63 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3232 77 None -81 63 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 3232 77 None -81 63 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 63153 17 None - 1 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 63153 17 None - 1 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 167494 76 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 167494 76 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 167494 76 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 204603 78 None 1 7 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 204603 78 None 1 7 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 112557 54 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 112557 54 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 660 48 None -9 9 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
374 660 48 None -9 9 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 660 48 None -9 9 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 660 48 None -9 9 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 660 48 None -9 9 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1643 108 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1643 108 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1643 108 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1643 108 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 1643 108 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 203596 102 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 203596 102 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 51640 43 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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 51640 43 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CHRM3 in an in vitro assay with cellular 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
316 2816 19 None 1 9 Rat 10.3 pEC50 = 10.3 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
317 2816 19 None 1 9 Rat 10.3 pEC50 = 10.3 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
71183 2816 19 None 1 9 Rat 10.3 pEC50 = 10.3 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL3140030 2816 19 None 1 9 Rat 10.3 pEC50 = 10.3 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL376897 2816 19 None 1 9 Rat 10.3 pEC50 = 10.3 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
DB00462 2816 19 None 1 9 Rat 10.3 pEC50 = 10.3 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
316 2816 19 None 1 9 Rat 9.7 pEC50 = 9.7 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
317 2816 19 None 1 9 Rat 9.7 pEC50 = 9.7 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
71183 2816 19 None 1 9 Rat 9.7 pEC50 = 9.7 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL3140030 2816 19 None 1 9 Rat 9.7 pEC50 = 9.7 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
CHEMBL376897 2816 19 None 1 9 Rat 9.7 pEC50 = 9.7 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
DB00462 2816 19 None 1 9 Rat 9.7 pEC50 = 9.7 Binding
Stimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometryStimulation of disulfide bond cross-linking formation in rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells by scanning densitometry
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1074/jbc.m704875200
367 3795 12 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
5487427 3795 12 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
8592 3795 12 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL1900528 3795 12 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL3305968 3795 12 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL4650755 3795 12 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
DB01409 3795 12 None 2 8 Human 9.4 pEC50 = 9.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
2230 464 60 None -588 10 Human 7.0 pEC50 = 7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00156a018
296 464 60 None -588 10 Human 7.0 pEC50 = 7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00156a018
CHEMBL7303 464 60 None -588 10 Human 7.0 pEC50 = 7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00156a018
DB04365 464 60 None -588 10 Human 7.0 pEC50 = 7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00156a018
9308 17722 21 None - 7 Human 6.0 pEC50 = 6 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
CHEMBL1255785 17722 21 None - 7 Human 6.0 pEC50 = 6 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
CHEMBL12587 17722 21 None - 7 Human 6.0 pEC50 = 6 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
CHEMBL292911 17722 21 None - 7 Human 6.0 pEC50 = 6 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
170332 160952 1 None -7 3 Human 5.0 pEC50 = 5 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4091934 160952 1 None -7 3 Human 5.0 pEC50 = 5 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115997 160952 1 None -7 3 Human 5.0 pEC50 = 5 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
91468 207041 15 None - 0 Human 5.0 pEC50 = 5.0 Binding
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 207041 15 None - 0 Human 5.0 pEC50 = 5.0 Binding
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 160952 1 None -7 3 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4091934 160952 1 None -7 3 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115997 160952 1 None -7 3 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
319 1312 44 None 2 9 Human 8.0 pEC50 = 8.0 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
321 1312 44 None 2 9 Human 8.0 pEC50 = 8.0 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031 1312 44 None 2 9 Human 8.0 pEC50 = 8.0 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
784 1312 44 None 2 9 Human 8.0 pEC50 = 8.0 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
CHEMBL1346 1312 44 None 2 9 Human 8.0 pEC50 = 8.0 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
DB00496 1312 44 None 2 9 Human 8.0 pEC50 = 8.0 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
13621561 11039 2 None - 0 Human 5.9 pEC50 = 5.9 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 178 2 1 4 0.3 C#CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1177918 11039 2 None - 0 Human 5.9 pEC50 = 5.9 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 178 2 1 4 0.3 C#CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL6767 11039 2 None - 0 Human 5.9 pEC50 = 5.9 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 178 2 1 4 0.3 C#CCOc1noc2c1CNCC2 10.1021/jm00156a018
10261985 203926 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL69306 203926 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
13621555 11912 3 None - 0 Human 4.9 pEC50 = 4.9 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 180 3 1 4 0.9 C=CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1182820 11912 3 None - 0 Human 4.9 pEC50 = 4.9 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 180 3 1 4 0.9 C=CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL268175 11912 3 None - 0 Human 4.9 pEC50 = 4.9 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 180 3 1 4 0.9 C=CCOc1noc2c1CNCC2 10.1021/jm00156a018
10465280 102758 1 None - 0 Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 196 2 1 4 1.5 CC(C)Oc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL305264 102758 1 None - 0 Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 196 2 1 4 1.5 CC(C)Oc1noc2c1CNCCC2 10.1021/jm00012a019
2166 3101 49 None -22 8 Human 5.8 pEC50 = 5.8 Binding
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 3101 49 None -22 8 Human 5.8 pEC50 = 5.8 Binding
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 3101 49 None -22 8 Human 5.8 pEC50 = 5.8 Binding
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 3101 49 None -22 8 Human 5.8 pEC50 = 5.8 Binding
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 3101 49 None -22 8 Human 5.8 pEC50 = 5.8 Binding
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 11921 2 None - 0 Human 5.8 pEC50 = 5.8 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCOc1noc2c1CN(C)CC2 10.1021/jm00156a018
CHEMBL1182850 11921 2 None - 0 Human 5.8 pEC50 = 5.8 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCOc1noc2c1CN(C)CC2 10.1021/jm00156a018
CHEMBL269706 11921 2 None - 0 Human 5.8 pEC50 = 5.8 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCOc1noc2c1CN(C)CC2 10.1021/jm00156a018
CHEMBL5287096 194590 0 None - 0 Human 4.8 pEC50 = 4.8 Binding
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 194590 0 None - 0 Human 4.8 pEC50 = 4.8 Binding
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
CHEMBL5284728 194237 0 None - 0 Human 4.8 pEC50 = 4.8 Binding
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 2957 17 None -89 6 Human 5.8 pEC50 = 5.8 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
4629 2957 17 None -89 6 Human 5.8 pEC50 = 5.8 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
8595 2957 17 None -89 6 Human 5.8 pEC50 = 5.8 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
CHEMBL44674 2957 17 None -89 6 Human 5.8 pEC50 = 5.8 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
125603 11034 10 None - 0 Human 5.8 pEC50 = 5.8 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 154 1 1 4 0.3 COc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1177907 11034 10 None - 0 Human 5.8 pEC50 = 5.8 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 154 1 1 4 0.3 COc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL6451 11034 10 None - 0 Human 5.8 pEC50 = 5.8 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 154 1 1 4 0.3 COc1noc2c1CNCC2 10.1021/jm00156a018
2551 791 23 None -346 11 Human 5.8 pEC50 = 5.8 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
298 791 23 None -346 11 Human 5.8 pEC50 = 5.8 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
488 791 23 None -346 11 Human 5.8 pEC50 = 5.8 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
CHEMBL965 791 23 None -346 11 Human 5.8 pEC50 = 5.8 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
DB00411 791 23 None -346 11 Human 5.8 pEC50 = 5.8 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
2551 791 23 None -346 11 Human 5.7 pEC50 = 5.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
298 791 23 None -346 11 Human 5.7 pEC50 = 5.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
488 791 23 None -346 11 Human 5.7 pEC50 = 5.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
CHEMBL965 791 23 None -346 11 Human 5.7 pEC50 = 5.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
DB00411 791 23 None -346 11 Human 5.7 pEC50 = 5.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
156009673 178230 0 None 1 3 Human 8.7 pEC50 = 8.7 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4633816 178230 0 None 1 3 Human 8.7 pEC50 = 8.7 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650683 178230 0 None 1 3 Human 8.7 pEC50 = 8.7 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
156014812 178238 0 None 1 3 Human 8.7 pEC50 = 8.7 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4647437 178238 0 None 1 3 Human 8.7 pEC50 = 8.7 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650736 178238 0 None 1 3 Human 8.7 pEC50 = 8.7 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
13621572 11036 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCN1CCc2onc(OC)c2C1 10.1021/jm00156a018
CHEMBL1177910 11036 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCN1CCc2onc(OC)c2C1 10.1021/jm00156a018
CHEMBL6568 11036 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 182 2 0 4 1.1 CCN1CCc2onc(OC)c2C1 10.1021/jm00156a018
CHEMBL5272950 193716 0 None - 0 Human 4.7 pEC50 = 4.7 Binding
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 791 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
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
298 791 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
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
488 791 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
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 791 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
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 791 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
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 2956 25 None -309 8 Human 6.7 pEC50 = 6.7 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
4630 2956 25 None -309 8 Human 6.7 pEC50 = 6.7 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
CHEMBL7634 2956 25 None -309 8 Human 6.7 pEC50 = 6.7 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
2551 791 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
298 791 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
488 791 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
CHEMBL965 791 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
DB00411 791 23 None -346 11 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
187 255 39 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 255 39 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 255 39 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 255 39 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 255 39 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 255 39 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
187 255 39 None -26 9 Human 6.7 pEC50 = 6.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
294 255 39 None -26 9 Human 6.7 pEC50 = 6.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
65 255 39 None -26 9 Human 6.7 pEC50 = 6.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
8593 255 39 None -26 9 Human 6.7 pEC50 = 6.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
CHEMBL667 255 39 None -26 9 Human 6.7 pEC50 = 6.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
DB03128 255 39 None -26 9 Human 6.7 pEC50 = 6.7 Binding
Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
187 255 39 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 255 39 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 255 39 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 255 39 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 255 39 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 255 39 None -26 9 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
187 255 39 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 255 39 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 255 39 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 255 39 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 255 39 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 255 39 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
2551 791 23 None -346 11 Human 7.6 pEC50 = 7.6 Binding
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
298 791 23 None -346 11 Human 7.6 pEC50 = 7.6 Binding
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
488 791 23 None -346 11 Human 7.6 pEC50 = 7.6 Binding
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 791 23 None -346 11 Human 7.6 pEC50 = 7.6 Binding
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 791 23 None -346 11 Human 7.6 pEC50 = 7.6 Binding
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 3610 51 None -1 8 Human 7.6 pEC50 = 7.6 Binding
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 3610 51 None -1 8 Human 7.6 pEC50 = 7.6 Binding
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 3610 51 None -1 8 Human 7.6 pEC50 = 7.6 Binding
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 3610 51 None -1 8 Human 7.6 pEC50 = 7.6 Binding
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 3610 51 None -1 8 Human 7.6 pEC50 = 7.6 Binding
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 39 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 255 39 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 255 39 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 255 39 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 255 39 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 255 39 None -26 9 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
156015097 177528 0 None 1 3 Human 7.6 pEC50 = 7.6 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4640324 177528 0 None 1 3 Human 7.6 pEC50 = 7.6 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
156015300 177568 0 None 4 3 Human 7.6 pEC50 = 7.6 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640703 177568 0 None 4 3 Human 7.6 pEC50 = 7.6 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
156021744 178090 0 None 1 3 Human 7.6 pEC50 = 7.6 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4648071 178090 0 None 1 3 Human 7.6 pEC50 = 7.6 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL5285668 194607 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
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 194607 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
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 97228 37 None - 0 Human 6.5 pEC50 = 6.5 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 141 1 1 3 0.1 COC(=O)C1=CCCNC1 10.1021/jm00156a018
CHEMBL268808 97228 37 None - 0 Human 6.5 pEC50 = 6.5 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 141 1 1 3 0.1 COC(=O)C1=CCCNC1 10.1021/jm00156a018
CHEMBL5277944 194639 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
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 194639 0 None - 0 Human 4.5 pEC50 = 4.5 Binding
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 464 60 None -588 10 Human 6.5 pEC50 = 6.5 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
296 464 60 None -588 10 Human 6.5 pEC50 = 6.5 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
CHEMBL7303 464 60 None -588 10 Human 6.5 pEC50 = 6.5 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
DB04365 464 60 None -588 10 Human 6.5 pEC50 = 6.5 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
13621545 11037 5 None - 0 Human 5.5 pEC50 = 5.5 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 2 1 4 0.7 CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1177913 11037 5 None - 0 Human 5.5 pEC50 = 5.5 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 2 1 4 0.7 CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL6680 11037 5 None - 0 Human 5.5 pEC50 = 5.5 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 2 1 4 0.7 CCOc1noc2c1CNCC2 10.1021/jm00156a018
137629935 160996 0 None -1 3 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4060823 160996 0 None -1 3 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116342 160996 0 None -1 3 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M3 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
156011965 177268 0 None 3 3 Human 8.4 pEC50 = 8.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636528 177268 0 None 3 3 Human 8.4 pEC50 = 8.4 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assayAntagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
13621565 11043 1 None - 0 Human 5.4 pEC50 = 5.4 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 192 2 1 4 0.7 CC#CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL1177927 11043 1 None - 0 Human 5.4 pEC50 = 5.4 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 192 2 1 4 0.7 CC#CCOc1noc2c1CNCC2 10.1021/jm00156a018
CHEMBL7018 11043 1 None - 0 Human 5.4 pEC50 = 5.4 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 192 2 1 4 0.7 CC#CCOc1noc2c1CNCC2 10.1021/jm00156a018
10442337 203925 2 None - 0 Human 6.3 pEC50 = 6.3 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 182 2 1 4 1.1 CCOc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL69305 203925 2 None - 0 Human 6.3 pEC50 = 6.3 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 182 2 1 4 1.1 CCOc1noc2c1CNCCC2 10.1021/jm00012a019
187 255 39 None -26 9 Human 6.3 pEC50 = 6.3 Binding
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 39 None -26 9 Human 6.3 pEC50 = 6.3 Binding
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 39 None -26 9 Human 6.3 pEC50 = 6.3 Binding
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 39 None -26 9 Human 6.3 pEC50 = 6.3 Binding
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 39 None -26 9 Human 6.3 pEC50 = 6.3 Binding
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 39 None -26 9 Human 6.3 pEC50 = 6.3 Binding
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 102581 9 None - 0 Human 6.2 pEC50 = 6.2 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 168 1 1 4 0.7 COc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL304142 102581 9 None - 0 Human 6.2 pEC50 = 6.2 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 168 1 1 4 0.7 COc1noc2c1CNCCC2 10.1021/jm00012a019
3008304 3992 52 None - 0 Human 5.2 pEC50 = 5.2 Binding
Positive allosteric modulation activity at muscarinic M3 receptorPositive allosteric modulation activity at muscarinic M3 receptor
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm201139r
7632 3992 52 None - 0 Human 5.2 pEC50 = 5.2 Binding
Positive allosteric modulation activity at muscarinic M3 receptorPositive allosteric modulation activity at muscarinic M3 receptor
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm201139r
CHEMBL523685 3992 52 None - 0 Human 5.2 pEC50 = 5.2 Binding
Positive allosteric modulation activity at muscarinic M3 receptorPositive allosteric modulation activity at muscarinic M3 receptor
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm201139r
2551 791 23 None -346 11 Human 7.2 pEC50 = 7.2 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
298 791 23 None -346 11 Human 7.2 pEC50 = 7.2 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
488 791 23 None -346 11 Human 7.2 pEC50 = 7.2 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
CHEMBL965 791 23 None -346 11 Human 7.2 pEC50 = 7.2 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
DB00411 791 23 None -346 11 Human 7.2 pEC50 = 7.2 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00156a018
13621567 98132 7 None - 0 Human 6.1 pEC50 = 6.1 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 1 0 4 0.7 COc1noc2c1CN(C)CC2 10.1021/jm00156a018
CHEMBL27384 98132 7 None - 0 Human 6.1 pEC50 = 6.1 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 1 0 4 0.7 COc1noc2c1CN(C)CC2 10.1021/jm00156a018
CHEMBL440085 98132 7 None - 0 Human 6.1 pEC50 = 6.1 Binding
Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropineContraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine
ChEMBL 168 1 0 4 0.7 COc1noc2c1CN(C)CC2 10.1021/jm00156a018
57400422 71602 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 330 4 0 2 3.9 C[C@@](C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924027 71602 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 330 4 0 2 3.9 C[C@@](C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1963462 71602 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 330 4 0 2 3.9 C[C@@](C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
24758141 103700 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 4 0 2 3.9 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087959 103700 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 4 0 2 3.9 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2013.09.092
367 3795 12 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
5487427 3795 12 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
8592 3795 12 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
CHEMBL1900528 3795 12 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
CHEMBL3305968 3795 12 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
CHEMBL4650755 3795 12 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
DB01409 3795 12 None 2 8 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2010.10.016
57392578 68718 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 487 7 0 4 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc(Cl)s3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921908 68718 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 487 7 0 4 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc(Cl)s3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395222 69119 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 5.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924040 69119 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 5.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545528 103608 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 453 7 0 4 5.5 O=C(O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)C1(c2cccs2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087230 103608 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 453 7 0 4 5.5 O=C(O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)C1(c2cccs2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545784 103612 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 475 7 0 4 6.1 O=C(O[C@H]1C[N+]2(CCCc3nc4ccccc4o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087235 103612 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 475 7 0 4 6.1 O=C(O[C@H]1C[N+]2(CCCc3nc4ccccc4o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
57401273 68717 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 525 7 0 3 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cccc(Br)c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921907 68717 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 525 7 0 3 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cccc(Br)c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57394170 68732 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 517 8 0 4 6.4 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cc4ccccc4s3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921925 68732 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 517 8 0 4 6.4 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cc4ccccc4s3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57394234 68742 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 483 9 0 5 5.1 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921935 68742 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 483 9 0 5 5.1 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
59179619 103702 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 327 3 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)C1(c2ccccc2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087961 103702 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 327 3 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)C1(c2ccccc2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545282 103709 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 440 6 0 3 6.0 Cc1ccc(CC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)s1 10.1016/j.bmcl.2013.09.092
CHEMBL3088081 103709 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 440 6 0 3 6.0 Cc1ccc(CC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)s1 10.1016/j.bmcl.2013.09.092
72545526 103713 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 8 0 3 5.8 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088086 103713 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 8 0 3 5.8 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
57390665 68724 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 462 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921917 68724 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 462 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395990 68744 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 501 9 0 5 5.2 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921937 68744 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 501 9 0 5 5.2 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546493 103698 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 473 6 0 4 6.2 O=C(O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)on3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087957 103698 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 473 6 0 4 6.2 O=C(O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)on3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
58348375 103703 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 333 3 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)C1(c2cccs2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088075 103703 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 333 3 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)C1(c2cccs2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545281 103708 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 420 6 0 2 5.6 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088080 103708 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 420 6 0 2 5.6 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
57395991 68752 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 500 7 1 5 4.4 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccc(F)c3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921945 68752 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 500 7 1 5 4.4 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccc(F)c3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57391636 68807 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 518 7 1 7 3.7 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cncc(Cl)n3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922053 68807 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 518 7 1 7 3.7 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cncc(Cl)n3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988645 69115 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 351 4 0 4 3.2 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924036 69115 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 351 4 0 4 3.2 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546026 103618 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 439 6 2 4 3.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cc[nH]n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087242 103618 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 439 6 2 4 3.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cc[nH]n1 10.1016/j.bmcl.2013.09.092
72543916 103690 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 485 6 1 5 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cncc(Cl)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087949 103690 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 485 6 1 5 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cncc(Cl)n1 10.1016/j.bmcl.2013.09.092
72546261 103693 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 447 5 0 4 5.7 O=C(O[C@H]1C[N+]2(Cc3nc4ccccc4o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087952 103693 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 447 5 0 4 5.7 O=C(O[C@H]1C[N+]2(Cc3nc4ccccc4o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
11434515 261 6 None -4 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
11519741 261 6 None -4 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
4484 261 6 None -4 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
7449 261 6 None -4 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
CHEMBL1194325 261 6 None -4 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
DB08897 261 6 None -4 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
44552684 68726 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 8 0 4 4.9 Cc1cc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)ccn1 10.1016/j.bmcl.2011.10.002
CHEMBL1921919 68726 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 8 0 4 4.9 Cc1cc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)ccn1 10.1016/j.bmcl.2011.10.002
57397792 68748 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 406 6 1 5 2.1 C[C@@](C(=O)O[C@H]1C[N+]2(CC(N)=O)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921941 68748 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 406 6 1 5 2.1 C[C@@](C(=O)O[C@H]1C[N+]2(CC(N)=O)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57401219 68753 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 7 1 5 3.6 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921946 68753 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 7 1 5 3.6 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57391775 69126 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 465 7 0 3 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccccc3F)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924049 69126 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 465 7 0 3 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccccc3F)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
11693 1814 16 None -1 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
3494 1814 16 None -1 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
4302 1814 16 None -1 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
7459 1814 16 None -1 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
CHEMBL1201335 1814 16 None -1 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
DB00986 1814 16 None -1 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2013.09.092
72545787 103615 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 467 6 1 3 5.1 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccc(F)c1 10.1016/j.bmcl.2013.09.092
CHEMBL3087238 103615 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 467 6 1 3 5.1 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccc(F)c1 10.1016/j.bmcl.2013.09.092
72545525 103712 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 8 0 3 5.6 O=C(O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088085 103712 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 8 0 3 5.6 O=C(O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
44517831 68716 4 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 465 7 0 3 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921904 68716 4 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 465 7 0 3 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395952 68720 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 491 7 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCC3=CC4CCOC4C=C3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921911 68720 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 491 7 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCC3=CC4CCOC4C=C3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397744 68725 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 468 8 0 5 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921918 68725 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 468 8 0 5 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccncc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57390720 68805 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 467 7 1 6 3.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccon3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922051 68805 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 467 7 1 6 3.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccon3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57403853 68808 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 488 6 0 5 5.2 Cc1ccc2nc(C[N+]34CCC(CC3)[C@@H](OC(=O)[C@](C)(c3ccccc3)N3CCCCC3)C4)oc2c1 10.1016/j.bmcl.2011.10.002
CHEMBL1922054 68808 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 488 6 0 5 5.2 Cc1ccc2nc(C[N+]34CCC(CC3)[C@@H](OC(=O)[C@](C)(c3ccccc3)N3CCCCC3)C4)oc2c1 10.1016/j.bmcl.2011.10.002
57398751 69106 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 471 7 0 4 5.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccccc3F)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924025 69106 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 471 7 0 4 5.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccccc3F)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545530 103609 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 449 7 0 3 5.7 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087232 103609 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 449 7 0 3 5.7 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
72546025 103617 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 454 6 1 5 4.3 Cc1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)no1 10.1016/j.bmcl.2013.09.092
CHEMBL3087241 103617 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 454 6 1 5 4.3 Cc1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)no1 10.1016/j.bmcl.2013.09.092
72546496 103631 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087362 103631 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccn1 10.1016/j.bmcl.2013.09.092
72546739 103636 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccncn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087367 103636 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccncn1 10.1016/j.bmcl.2013.09.092
72546991 103637 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccnn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087368 103637 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccnn1 10.1016/j.bmcl.2013.09.092
72546262 103694 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 474 6 0 5 5.6 O=C(O[C@H]1C[N+]2(Cc3nc(-c4ccccc4)no3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087953 103694 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 474 6 0 5 5.6 O=C(O[C@H]1C[N+]2(Cc3nc(-c4ccccc4)no3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545285 103711 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 436 7 0 3 5.4 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088084 103711 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 436 7 0 3 5.4 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
11434515 261 6 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
11519741 261 6 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
4484 261 6 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
7449 261 6 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
CHEMBL1194325 261 6 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
DB08897 261 6 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
10143956 13879 0 None -1 3 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL1196359 13879 0 None -1 3 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL556635 13879 0 None -1 3 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
57390766 68719 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 497 7 0 3 5.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc4ccccc4c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921910 68719 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 497 7 0 3 5.9 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3ccc4ccccc4c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57402931 68723 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 459 7 0 4 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCC3CCCCC3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921914 68723 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 459 7 0 4 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCC3CCCCC3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57399407 68734 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 475 9 0 3 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921927 68734 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 475 9 0 3 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57401217 68747 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 400 6 1 4 2.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(N)=O)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921940 68747 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 400 6 1 4 2.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(N)=O)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397793 68749 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 7 1 4 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921942 68749 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 7 1 4 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57401218 68750 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 482 7 1 5 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921943 68750 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 482 7 1 5 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397794 68751 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 494 7 1 4 4.3 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccc(F)c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921944 68751 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 494 7 1 4 4.3 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccc(F)c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57392520 68804 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cnccn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922050 68804 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cnccn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57392521 68806 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 473 7 1 7 3.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccon3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922052 68806 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 473 7 1 7 3.2 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccon3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395096 68809 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 500 7 0 5 5.4 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)on3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922055 68809 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 500 7 0 5 5.4 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)on3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545785 103613 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 373 5 1 3 2.9 NC(=O)C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2 10.1016/j.bmcl.2013.09.092
CHEMBL3087236 103613 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 373 5 1 3 2.9 NC(=O)C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2 10.1016/j.bmcl.2013.09.092
72546736 103633 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccnc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087364 103633 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccnc1 10.1016/j.bmcl.2013.09.092
72547500 103687 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 485 6 1 5 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(Cl)nn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087946 103687 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 485 6 1 5 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(Cl)nn1 10.1016/j.bmcl.2013.09.092
10165877 63100 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779133 63100 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789396 63100 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
11852298 13994 0 None -1 3 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1197251 13994 0 None -1 3 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL564057 13994 0 None -1 3 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
71524764 144415 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 833 16 5 14 6.5 COc1cc(-c2noc(CCCN(C)[C@H]3CC[C@H](OC(=O)C(O)(c4cccs4)c4cccs4)CC3)n2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3906438 144415 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 833 16 5 14 6.5 COc1cc(-c2noc(CCCN(C)[C@H]3CC[C@H](OC(=O)C(O)(c4cccs4)c4cccs4)CC3)n2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
54592025 147970 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 695 18 5 10 6.4 CN(CCCCCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3934254 147970 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 695 18 5 10 6.4 CN(CCCCCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
44232927 195314 8 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 349 4 1 6 2.7 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL551729 195314 8 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 349 4 1 6 2.7 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
86765983 145789 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 342 4 0 2 4.1 C[C@@](C(=O)O[C@@H]1CC2CCC1[N+]2(C)C)(c1ccccc1)C1CCCC1 nan
CHEMBL3917058 145789 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 342 4 0 2 4.1 C[C@@](C(=O)O[C@@H]1CC2CCC1[N+]2(C)C)(c1ccccc1)C1CCCC1 nan
44233401 13592 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 10.1021/jm900132z
CHEMBL1194321 13592 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 10.1021/jm900132z
CHEMBL551327 13592 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 10.1021/jm900132z
44233177 13868 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL1196246 13868 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL556221 13868 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 10.1021/jm900132z
44233403 13869 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL1196247 13869 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL556222 13869 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
53372934 129274 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670826 129274 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
53372936 129275 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670827 129275 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
11693 1814 16 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
3494 1814 16 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
4302 1814 16 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
7459 1814 16 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
CHEMBL1201335 1814 16 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
DB00986 1814 16 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
11693 1814 16 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
3494 1814 16 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
4302 1814 16 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
7459 1814 16 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
CHEMBL1201335 1814 16 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
DB00986 1814 16 None -1 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2011.10.002
57392462 68735 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 481 9 0 4 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921928 68735 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 481 9 0 4 5.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57400294 68812 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 507 7 0 7 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3noc(-c4ccccc4)n3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922058 68812 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 507 7 0 7 4.9 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3noc(-c4ccccc4)n3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988644 69108 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 345 4 0 3 3.2 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924029 69108 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 345 4 0 3 3.2 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545786 103614 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 449 6 1 3 5.0 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087237 103614 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 449 6 1 3 5.0 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccc1 10.1016/j.bmcl.2013.09.092
72546993 103638 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 468 6 1 4 4.5 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncccc1F 10.1016/j.bmcl.2013.09.092
CHEMBL3087370 103638 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 468 6 1 4 4.5 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncccc1F 10.1016/j.bmcl.2013.09.092
72547254 103643 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 518 6 1 4 5.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(C(F)(F)F)nc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087375 103643 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 518 6 1 4 5.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(C(F)(F)F)nc1 10.1016/j.bmcl.2013.09.092
72546263 103695 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 473 6 0 4 6.2 O=C(O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)no3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087954 103695 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 473 6 0 4 6.2 O=C(O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)no3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
69167248 103701 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 3 0 2 4.1 C[N+]1(C)CCC(OC(=O)C2(c3ccccc3)CCCCCC2)CC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087960 103701 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 3 0 2 4.1 C[N+]1(C)CCC(OC(=O)C2(c3ccccc3)CCCCCC2)CC1 10.1016/j.bmcl.2013.09.092
44236101 13996 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL1197261 13996 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL564515 13996 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
10208897 63097 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 455 8 0 2 6.1 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779049 63097 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 455 8 0 2 6.1 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789387 63097 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 455 8 0 2 6.1 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
10143718 63104 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779131 63104 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789435 63104 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 463 8 0 4 5.6 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
71558563 143755 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 758 14 5 13 5.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3900995 143755 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 758 14 5 13 5.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
54673357 145588 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 795 17 5 12 6.7 COc1cc(OCCCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3915601 145588 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 795 17 5 12 6.7 COc1cc(OCCCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
53372938 129276 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670828 129276 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
1734 116 10 None 1 13 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
307 116 10 None 1 13 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
CHEMBL168067 116 10 None 1 13 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
11569908 13969 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL1197028 13969 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL559106 13969 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
44232930 196670 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 343 4 1 5 2.6 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL564747 196670 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 343 4 1 5 2.6 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
57399406 68728 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 462 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cccnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921921 68728 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 462 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cccnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397746 68731 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 502 8 0 5 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3nc4ccccc4o3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921924 68731 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 502 8 0 5 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3nc4ccccc4o3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57394233 68739 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 8 0 4 4.9 Cc1ccc(OCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cc1 10.1016/j.bmcl.2011.10.002
CHEMBL1921932 68739 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 8 0 4 4.9 Cc1ccc(OCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cc1 10.1016/j.bmcl.2011.10.002
57395097 68810 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 501 7 0 6 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3nc(-c4ccccc4)no3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922056 68810 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 501 7 0 6 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3nc(-c4ccccc4)no3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546494 103699 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 474 6 0 5 5.6 O=C(O[C@H]1C[N+]2(Cc3nnc(-c4ccccc4)o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087958 103699 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 474 6 0 5 5.6 O=C(O[C@H]1C[N+]2(Cc3nnc(-c4ccccc4)o3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
367 3795 12 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
5487427 3795 12 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
8592 3795 12 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL1900528 3795 12 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL3305968 3795 12 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL4650755 3795 12 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
DB01409 3795 12 None 2 8 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
20735153 13591 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1194314 13591 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL551063 13591 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1021/jm900132z
11489419 13586 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 448 10 1 5 5.2 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
CHEMBL1194274 13586 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 448 10 1 5 5.2 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
CHEMBL549784 13586 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 448 10 1 5 5.2 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
44232931 196358 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 4 1 5 2.8 O=C(O[C@H]1CN2CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL562642 196358 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 4 1 5 2.8 O=C(O[C@H]1CN2CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
57390666 68733 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 518 8 0 5 5.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccc4ncsc4c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921926 68733 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 518 8 0 5 5.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3ccc4ncsc4c3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57396866 68811 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 506 7 0 6 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)no3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922057 68811 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 506 7 0 6 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(Cc3cc(-c4ccccc4)no3)CCC1CC2)(c1cccs1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546028 103620 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 457 6 1 6 3.9 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncns1 10.1016/j.bmcl.2013.09.092
CHEMBL3087244 103620 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 457 6 1 6 3.9 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncns1 10.1016/j.bmcl.2013.09.092
72547256 103645 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1nccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087377 103645 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1nccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
72546264 103696 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 472 6 0 4 5.8 O=C(O[C@H]1C[N+]2(Cc3ccn(-c4ccccc4)n3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087955 103696 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 472 6 0 4 5.8 O=C(O[C@H]1C[N+]2(Cc3ccn(-c4ccccc4)n3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
367 3795 12 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
5487427 3795 12 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
8592 3795 12 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
CHEMBL1900528 3795 12 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
CHEMBL3305968 3795 12 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
CHEMBL4650755 3795 12 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
DB01409 3795 12 None 2 8 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2015.02.065
71556977 142519 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 769 15 5 13 5.9 CN(CCCc1nc(-c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)no1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3890898 142519 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 769 15 5 13 5.9 CN(CCCc1nc(-c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)no1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
71566009 144282 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 838 17 5 13 5.4 COc1cc(OCC(=O)N(C)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3905320 144282 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 838 17 5 13 5.4 COc1cc(OCC(=O)N(C)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
71558416 151303 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 757 14 6 12 4.9 CN(CCCn1c(=O)[nH]c2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3961014 151303 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 757 14 6 12 4.9 CN(CCCn1c(=O)[nH]c2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
121347973 151604 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 732 14 5 13 4.6 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4c3OCC(=O)N4)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
CHEMBL3963770 151604 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 732 14 5 13 4.6 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4c3OCC(=O)N4)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
1734 116 10 None 1 13 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
307 116 10 None 1 13 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
CHEMBL168067 116 10 None 1 13 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
1734 116 10 None 1 13 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
307 116 10 None 1 13 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
CHEMBL168067 116 10 None 1 13 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
44236098 195625 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 343 4 1 5 2.6 O=C(O[C@H]1CN2CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL556426 195625 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 343 4 1 5 2.6 O=C(O[C@H]1CN2CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
1734 116 10 None 1 13 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
307 116 10 None 1 13 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
CHEMBL168067 116 10 None 1 13 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
44236340 13760 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1195513 13760 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL554725 13760 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
44232685 13997 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL1197273 13997 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
CHEMBL564765 13997 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1ccccc1)c1cccs1 10.1021/jm900132z
10119939 63098 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1777827 63098 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789388 63098 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
71558718 144697 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 14 5 13 5.7 CN(CCCn1c(=O)sc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3908788 144697 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 14 5 13 5.7 CN(CCCn1c(=O)sc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
57392515 68746 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 491 10 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOCCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921939 68746 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 491 10 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOCCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72545783 103611 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 438 7 0 4 4.7 Cn1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087234 103611 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 438 7 0 4 4.7 Cn1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
72546994 103639 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)nc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087371 103639 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)nc1 10.1016/j.bmcl.2013.09.092
1734 116 10 None 1 13 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
307 116 10 None 1 13 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
CHEMBL168067 116 10 None 1 13 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
44232681 13983 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 0 5 5.7 CC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1197156 13983 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 0 5 5.7 CC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL561187 13983 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 482 9 0 5 5.7 CC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)c1cccs1 10.1021/jm900132z
1734 116 10 None 1 13 Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
307 116 10 None 1 13 Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
CHEMBL168067 116 10 None 1 13 Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
9928017 62309 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 342 4 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779033 62309 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 342 4 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccs1)c1ccccc1 10.1016/j.bmcl.2011.03.096
10229167 63095 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 427 9 0 3 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779136 63095 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 427 9 0 3 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789385 63095 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 427 9 0 3 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
10393952 63099 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 529 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779140 63099 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 529 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1789389 63099 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 529 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
10187216 63108 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 461 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779128 63108 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 461 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789452 63108 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 461 8 0 3 6.1 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
10143858 63109 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779132 63109 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789454 63109 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 467 8 0 4 6.2 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
44236336 13981 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 364 4 1 5 2.8 C[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
CHEMBL1197131 13981 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 364 4 1 5 2.8 C[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
CHEMBL560327 13981 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 364 4 1 5 2.8 C[N+]12CCC(CC1)[C@@H](OC(=O)C(O)(c1cccs1)c1cccs1)C2 10.1021/jm900132z
71558567 142656 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 740 14 5 11 6.2 CN(CCCn1ccc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3892021 142656 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 740 14 5 11 6.2 CN(CCCn1ccc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
121347950 151208 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 728 14 5 12 5.1 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
CHEMBL3960091 151208 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 728 14 5 12 5.1 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
44232683 13594 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
CHEMBL1194336 13594 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
CHEMBL551731 13594 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
57399408 68736 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 463 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921929 68736 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 463 8 0 4 4.6 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57395989 68743 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 495 9 0 4 5.1 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921936 68743 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 495 9 0 4 5.1 C[C@@](C(=O)O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57391773 69125 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 425 7 0 3 4.9 CC(C)=CCC[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
CHEMBL1924046 69125 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 425 7 0 3 4.9 CC(C)=CCC[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
72546738 103635 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cncnc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087366 103635 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 451 6 1 5 3.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cncnc1 10.1016/j.bmcl.2013.09.092
72546995 103640 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 468 6 1 4 4.5 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(F)cn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087372 103640 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 468 6 1 4 4.5 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(F)cn1 10.1016/j.bmcl.2013.09.092
72543915 103689 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cncc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087948 103689 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cncc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)n1 10.1016/j.bmcl.2013.09.092
10007638 120850 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 8 2 4 4.4 O=C(N[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401648 120850 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 8 2 4 4.4 O=C(N[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559195 120850 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 8 2 4 4.4 O=C(N[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
67548926 120852 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 473 8 2 5 4.5 O=C(N[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401649 120852 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 473 8 2 5 4.5 O=C(N[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559201 120852 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 473 8 2 5 4.5 O=C(N[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
10325942 120853 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 8 2 5 3.9 O=C(N[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401650 120853 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 8 2 5 3.9 O=C(N[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559202 120853 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 8 2 5 3.9 O=C(N[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
44236099 195532 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 4 1 5 2.8 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL554699 195532 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 4 1 5 2.8 O=C(O[C@H]1CN2CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
54673354 148702 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 808 16 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3940214 148702 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 808 16 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
44236332 13985 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL1197183 13985 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL561870 13985 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
72548703 161543 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor after 60 mins by scintillation counting analysisDisplacement of [3H]4-DAMP from human recombinant M3 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161543 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor after 60 mins by scintillation counting analysisDisplacement of [3H]4-DAMP from human recombinant M3 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
939077 195045 2 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 2 0 4 3.6 O=C(O[C@H]1CN2CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL549577 195045 2 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 2 0 4 3.6 O=C(O[C@H]1CN2CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1021/jm900132z
57397791 68745 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921938 68745 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57402222 69109 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 353 4 0 3 3.6 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1C=CC=CC=C1 10.1016/j.bmcl.2011.10.002
CHEMBL1924030 69109 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 353 4 0 3 3.6 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1C=CC=CC=C1 10.1016/j.bmcl.2011.10.002
57397002 69110 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 363 4 0 4 2.7 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCSCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924031 69110 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 363 4 0 4 2.7 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCSCC1 10.1016/j.bmcl.2011.10.002
72547252 103641 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccnc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c1 10.1016/j.bmcl.2013.09.092
CHEMBL3087373 103641 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccnc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c1 10.1016/j.bmcl.2013.09.092
72547255 103644 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087376 103644 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 464 6 1 4 4.7 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
72547498 103647 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)nn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087379 103647 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1ccc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)nn1 10.1016/j.bmcl.2013.09.092
72547501 103688 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cnc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087947 103688 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cnc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cn1 10.1016/j.bmcl.2013.09.092
11678378 120860 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 7 1 3 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2015.02.065
CHEMBL3401654 120860 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 7 1 3 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2015.02.065
CHEMBL3559211 120860 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 469 7 1 3 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2015.02.065
10164137 63096 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 423 9 0 3 5.1 CCCCN(C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779137 63096 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 423 9 0 3 5.1 CCCCN(C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789386 63096 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 423 9 0 3 5.1 CCCCN(C(=O)O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
10300661 63107 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 421 9 0 2 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779135 63107 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 421 9 0 2 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789451 63107 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 421 9 0 2 5.7 CCCCN(C(=O)O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
117628769 145001 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 772 15 5 13 5.2 CN(CCCn1c(=O)oc2cc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3911114 145001 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 772 15 5 13 5.2 CN(CCCn1c(=O)oc2cc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
54586745 63110 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 523 8 0 2 6.8 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCCc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779138 63110 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 523 8 0 2 6.8 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCCc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1789461 63110 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 523 8 0 2 6.8 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCCc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
688566 195860 24 None - 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 337 4 1 4 2.6 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
CHEMBL558910 195860 24 None - 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 337 4 1 4 2.6 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm900132z
44235871 196549 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 2 1 4 2.5 O=C(O[C@H]1CN2CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL563887 196549 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 335 2 1 4 2.5 O=C(O[C@H]1CN2CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
44236334 13980 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL1197117 13980 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL559931 13980 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 10.1021/jm900132z
9946010 62310 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 342 4 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779034 62310 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 342 4 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccsc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
10208972 63102 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 457 8 0 3 5.5 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779129 63102 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 457 8 0 3 5.5 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789429 63102 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 457 8 0 3 5.5 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
57390714 68740 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 8 0 4 4.9 Cc1cccc(OCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)c1 10.1016/j.bmcl.2011.10.002
CHEMBL1921933 68740 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 8 0 4 4.9 Cc1cccc(OCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)c1 10.1016/j.bmcl.2011.10.002
57395997 68803 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccnn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922049 68803 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3cccnn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988641 69112 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 359 4 0 3 3.4 CC1CCN(C(C)(C(=O)OC2CC[N+](C)(C)CC2)c2ccccc2)CC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924033 69112 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 359 4 0 3 3.4 CC1CCN(C(C)(C(=O)OC2CC[N+](C)(C)CC2)c2ccccc2)CC1 10.1016/j.bmcl.2011.10.002
57403964 69121 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 385 5 0 3 3.9 CC(C)[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
CHEMBL1924042 69121 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 385 5 0 3 3.9 CC(C)[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
72545782 103610 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 463 7 0 3 6.0 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c(C)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087233 103610 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 463 7 0 3 6.0 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c(C)n1 10.1016/j.bmcl.2013.09.092
72547497 103646 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)ncn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087378 103646 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 465 6 1 5 4.1 Cc1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)ncn1 10.1016/j.bmcl.2013.09.092
71565927 146636 0 None - 0 Human 9.0 pIC50 = 9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 758 12 4 11 6.3 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C2(C)c3ccccc3Oc3ccccc32)CC1 nan
CHEMBL3923686 146636 0 None - 0 Human 9.0 pIC50 = 9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 758 12 4 11 6.3 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C2(C)c3ccccc3Oc3ccccc32)CC1 nan
54672858 151449 0 None - 0 Human 9.0 pIC50 = 9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 794 16 7 12 5.9 COc1cc(NC(=O)CCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3962171 151449 0 None - 0 Human 9.0 pIC50 = 9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 794 16 7 12 5.9 COc1cc(NC(=O)CCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
44233175 13987 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL1197209 13987 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
CHEMBL562655 13987 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1021/jm900132z
44233173 13988 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL1197216 13988 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
CHEMBL562890 13988 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 10.1021/jm900132z
316 2816 19 None -2 9 Human 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
317 2816 19 None -2 9 Human 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
71183 2816 19 None -2 9 Human 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
CHEMBL3140030 2816 19 None -2 9 Human 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
CHEMBL376897 2816 19 None -2 9 Human 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
DB00462 2816 19 None -2 9 Human 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/s0960-894x(98)00351-5
10246307 117752 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 4 2 4 2.3 O=C(N[C@H]1CN2CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1016/j.bmcl.2015.02.065
CHEMBL3401643 117752 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 4 2 4 2.3 O=C(N[C@H]1CN2CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1016/j.bmcl.2015.02.065
54590925 153289 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 794 15 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3978112 153289 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 794 15 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
49800047 14451 1 None -2 5 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
CHEMBL1201024 14451 1 None -2 5 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
CHEMBL1201268 14451 1 None -2 5 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
9967590 62111 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 336 4 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1777826 62111 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 336 4 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
54582845 63101 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 525 8 0 3 6.2 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCOc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779139 63101 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 525 8 0 3 6.2 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCOc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1789405 63101 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 525 8 0 3 6.2 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2C[N+]3(CCOc4ccccc4)CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
50925542 19145 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4cccc(Cl)c4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289653 19145 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4cccc(Cl)c4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
57401170 68729 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 8 0 4 4.9 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cn1 10.1016/j.bmcl.2011.10.002
CHEMBL1921922 68729 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 476 8 0 4 4.9 Cc1ccc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cn1 10.1016/j.bmcl.2011.10.002
57397790 68738 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 497 8 0 4 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccc(Cl)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921931 68738 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 497 8 0 4 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccc(Cl)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57402970 68802 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccncn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1922048 68802 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 478 7 1 6 3.0 C[C@@](C(=O)O[C@H]1C[N+]2(CC(=O)Nc3ccncn3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988643 69111 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 381 4 0 3 3.4 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCC(F)(F)CC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924032 69111 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 381 4 0 3 3.4 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCC(F)(F)CC1 10.1016/j.bmcl.2011.10.002
1201549 594 24 None -1 20 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 594 24 None -1 20 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 594 24 None -1 20 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 594 24 None -1 20 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 594 24 None -1 20 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 594 24 None -1 20 Human 8.9 pIC50 = 8.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
54592027 143968 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 717 15 5 11 5.3 CN(CCOc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3902803 143968 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 717 15 5 11 5.3 CN(CCOc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
54583840 62321 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 404 4 0 3 4.7 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2CN3CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779045 62321 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 404 4 0 3 4.7 Cc1cccc(N(Cc2cc(F)c(F)cc2F)C(=O)O[C@H]2CN3CCC2CC3)c1 10.1016/j.bmcl.2011.03.096
118638354 145562 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 17 5 11 5.3 CN(CCN(C)[C@H]1CC[C@H](OC(C(=O)O)(c2cccs2)c2cccs2)CC1)C(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 nan
CHEMBL3915401 145562 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 17 5 11 5.3 CN(CCN(C)[C@H]1CC[C@H](OC(C(=O)O)(c2cccs2)c2cccs2)CC1)C(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 nan
54673189 149138 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 801 15 6 14 5.3 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(C#N)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3943564 149138 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 801 15 6 14 5.3 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(C#N)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
25147683 62322 37 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 408 4 0 3 4.5 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779046 62322 37 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 408 4 0 3 4.5 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cc(F)c(F)c(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
10372836 102370 39 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
CHEMBL3039518 102370 39 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
54591014 145745 3 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
CHEMBL3916700 145745 3 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
71558565 167416 9 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 742 14 5 13 5.0 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 10.1021/acs.jmedchem.8b01520
CHEMBL4297483 167416 9 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 742 14 5 13 5.0 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 10.1021/acs.jmedchem.8b01520
155531077 171596 2 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 669 10 4 10 4.4 CC(C)c1ncc(C(=O)N2CCOC3(CCN(Cc4ccc(F)c(CCNC[C@H](O)c5ccc(O)c6[nH]c(=O)sc56)c4)CC3)C2)s1 10.1021/acs.jmedchem.8b01520
CHEMBL4465556 171596 2 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at human M3 receptorAntagonist activity at human M3 receptor
ChEMBL 669 10 4 10 4.4 CC(C)c1ncc(C(=O)N2CCOC3(CCN(Cc4ccc(F)c(CCNC[C@H](O)c5ccc(O)c6[nH]c(=O)sc56)c4)CC3)C2)s1 10.1021/acs.jmedchem.8b01520
57397743 68722 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 486 7 1 3 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3c[nH]c4ccccc34)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921913 68722 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 486 7 1 3 5.3 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3c[nH]c4ccccc34)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57393499 71569 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 316 4 0 2 3.5 CC(C(=O)O[C@@H]1CC[N+](C)(C)C1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924026 71569 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 316 4 0 2 3.5 CC(C(=O)O[C@@H]1CC[N+](C)(C)C1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1963231 71569 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 316 4 0 2 3.5 CC(C(=O)O[C@@H]1CC[N+](C)(C)C1)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2011.10.002
54591014 145745 3 None - 0 Human 8.8 pIC50 = 8.8 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3916700 145745 3 None - 0 Human 8.8 pIC50 = 8.8 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
54673020 151562 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 766 14 6 11 5.5 CN(CCC(=O)Nc1cc(F)c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1F)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3963417 151562 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 766 14 6 11 5.5 CN(CCC(=O)Nc1cc(F)c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1F)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
10143954 13587 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL1194286 13587 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL549986 13587 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
11306852 13993 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 434 8 1 3 5.0 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C1(O)c3ccccc3-c3ccccc31)C2 10.1021/jm900132z
CHEMBL1197250 13993 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 434 8 1 3 5.0 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C1(O)c3ccccc3-c3ccccc31)C2 10.1021/jm900132z
CHEMBL563996 13993 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 434 8 1 3 5.0 CCCCCCC[N+]12CCC(CC1)[C@@H](OC(=O)C1(O)c3ccccc3-c3ccccc31)C2 10.1021/jm900132z
25897919 55622 14 None 1 8 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2015.02.065
657309 55622 14 None 1 8 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2015.02.065
CHEMBL1464005 55622 14 None 1 8 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2015.02.065
CHEMBL1621597 55622 14 None 1 8 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2015.02.065
9944783 62313 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 316 6 0 3 3.9 CCCCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779037 62313 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 316 6 0 3 3.9 CCCCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
54673702 149607 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 814 15 6 14 5.6 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2c1OCC(=O)N2 nan
CHEMBL3947244 149607 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 814 15 6 14 5.6 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2c1OCC(=O)N2 nan
1734 116 10 None 1 13 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2010.07.034
307 116 10 None 1 13 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2010.07.034
CHEMBL168067 116 10 None 1 13 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2010.07.034
46890906 7010 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 329 5 2 2 4.8 OC(CCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1084850 7010 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 329 5 2 2 4.8 OC(CCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
50925541 19127 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289545 19127 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
57393500 69113 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 305 4 0 3 2.2 CN(C)C(C)(C(=O)OC1CC[N+](C)(C)CC1)c1ccccc1 10.1016/j.bmcl.2011.10.002
CHEMBL1924034 69113 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 305 4 0 3 2.2 CN(C)C(C)(C(=O)OC1CC[N+](C)(C)CC1)c1ccccc1 10.1016/j.bmcl.2011.10.002
72546495 103630 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 496 6 1 5 5.3 CC(C)(C)c1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)no1 10.1016/j.bmcl.2013.09.092
CHEMBL3087361 103630 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 496 6 1 5 5.3 CC(C)(C)c1cc(NC(=O)C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)no1 10.1016/j.bmcl.2013.09.092
102514695 181814 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]N -methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells incubated for 90 mins by scintillation counting methodDisplacement of [3H]N -methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells incubated for 90 mins by scintillation counting method
ChEMBL 970 18 0 10 9.4 O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)C1CN(C(=O)c2ccc(COc3cccc(CN(C(=O)O[C@H]4CN5CCC4CC5)c4ccccc4)c3)cc2)C1 10.1021/acs.jmedchem.9b02170
CHEMBL4778407 181814 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]N -methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells incubated for 90 mins by scintillation counting methodDisplacement of [3H]N -methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells incubated for 90 mins by scintillation counting method
ChEMBL 970 18 0 10 9.4 O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)C1CN(C(=O)c2ccc(COc3cccc(CN(C(=O)O[C@H]4CN5CCC4CC5)c4ccccc4)c3)cc2)C1 10.1021/acs.jmedchem.9b02170
52947552 19075 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 404 4 1 5 2.9 O=C(c1ccc(CO)o1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289201 19075 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 404 4 1 5 2.9 O=C(c1ccc(CO)o1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
52942458 19215 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 382 3 0 2 4.9 O=C(c1ccccc1)N1CCC2(CCN(Cc3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2010.10.016
CHEMBL1290183 19215 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 382 3 0 2 4.9 O=C(c1ccccc1)N1CCC2(CCN(Cc3cccc(Cl)c3)CC2)CC1 10.1016/j.bmcl.2010.10.016
52947320 19216 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 362 3 0 2 4.5 Cc1cccc(CN2CCC3(CC2)CCN(C(=O)c2ccccc2)CC3)c1 10.1016/j.bmcl.2010.10.016
CHEMBL1290184 19216 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 362 3 0 2 4.5 Cc1cccc(CN2CCC3(CC2)CCN(C(=O)c2ccccc2)CC3)c1 10.1016/j.bmcl.2010.10.016
72546023 103616 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 443 5 0 4 3.2 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)N1CCOCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087239 103616 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 443 5 0 4 3.2 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)N1CCOCC1 10.1016/j.bmcl.2013.09.092
9974222 11889 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1182709 11889 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL262198 11889 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
13578551 101257 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 7 1 5 3.9 CCN(CC)CCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL296405 101257 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 7 1 5 3.9 CCN(CC)CCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
13578548 101335 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 393 4 1 5 2.7 CN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL296988 101335 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 393 4 1 5 2.7 CN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
10094518 101366 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(C)cc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL297224 101366 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(C)cc2C(=O)Nc2cccnc21 10.1021/jm00128a008
46871665 6563 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1F 10.1016/j.bmcl.2010.04.128
CHEMBL1083108 6563 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1F 10.1016/j.bmcl.2010.04.128
13578551 101257 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 7 1 5 3.9 CCN(CC)CCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL296405 101257 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 7 1 5 3.9 CCN(CC)CCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
13578548 101335 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 393 4 1 5 2.7 CN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL296988 101335 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 393 4 1 5 2.7 CN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
10094518 101366 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(C)cc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL297224 101366 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(C)cc2C(=O)Nc2cccnc21 10.1021/jm00048a014
107867 2953 55 None -12 11 Rat 5.0 pIC50 = 5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00128a008
309 2953 55 None -12 11 Rat 5.0 pIC50 = 5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00128a008
CHEMBL17045 2953 55 None -12 11 Rat 5.0 pIC50 = 5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00128a008
46891141 6530 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 374 5 2 2 4.5 CC[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083002 6530 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 374 5 2 2 4.5 CC[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46891142 6531 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 364 4 2 2 3.8 O=C(NC[C@H]1CCNC[C@H]1F)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083003 6531 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 364 4 2 2 3.8 O=C(NC[C@H]1CCNC[C@H]1F)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46891143 6604 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 396 4 2 2 4.7 O=C(NCC1=C(F)CNCC1)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
CHEMBL1083317 6604 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 396 4 2 2 4.7 O=C(NCC1=C(F)CNCC1)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
107867 2953 55 None -12 11 Rat 5.0 pIC50 = 5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00048a014
309 2953 55 None -12 11 Rat 5.0 pIC50 = 5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00048a014
CHEMBL17045 2953 55 None -12 11 Rat 5.0 pIC50 = 5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00048a014
14660293 52623 3 None - 0 Human 4.0 pIC50 = 4 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 191 0 1 4 1.3 c1cc2nsnc2c2c1CCNC2 10.1021/jm9705216
CHEMBL15936 52623 3 None - 0 Human 4.0 pIC50 = 4 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 191 0 1 4 1.3 c1cc2nsnc2c2c1CCNC2 10.1021/jm9705216
44302755 202653 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 408 4 1 6 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL61494 202653 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 408 4 1 6 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
10020681 117757 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 348 4 2 5 2.3 O=C(N[C@@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401657 117757 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 348 4 2 5 2.3 O=C(N[C@@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
44302727 101891 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccc(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL300987 101891 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccc(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
10782462 12082 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1184068 12082 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL330999 12082 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
10592484 11403 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.5 CCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180314 11403 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.5 CCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL121476 11403 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.5 CCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
44233173 13988 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
CHEMBL1197216 13988 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
CHEMBL562890 13988 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 486 7 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
9996901 117751 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 4 1 4 3.2 O=C(N[C@H]1CN2CCC1CC2)C(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401642 117751 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 332 4 1 4 3.2 O=C(N[C@H]1CN2CCC1CC2)C(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
135494454 172731 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 785 25 5 11 6.7 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL450986 172731 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 785 25 5 11 6.7 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
24739886 187845 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 469 6 1 3 4.2 NC(=O)CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
CHEMBL496376 187845 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 469 6 1 3 4.2 NC(=O)CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
2230 464 60 None -588 10 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
296 464 60 None -588 10 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
CHEMBL7303 464 60 None -588 10 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
DB04365 464 60 None -588 10 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9702903
10641009 11394 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180292 11394 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL120472 11394 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
72546260 103621 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 440 6 1 5 4.0 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncco1 10.1016/j.bmcl.2013.09.092
CHEMBL3087245 103621 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 440 6 1 5 4.0 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ncco1 10.1016/j.bmcl.2013.09.092
46890907 7011 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 311 4 1 1 5.4 Clc1cccc(-c2ccccc2/C=C/CC2CCNCC2)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1084851 7011 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 311 4 1 1 5.4 Clc1cccc(-c2ccccc2/C=C/CC2CCNCC2)c1 10.1016/j.bmcl.2010.04.127
10511551 25799 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@@H]1CN2CC[C@H]1C2 10.1021/jm9702903
CHEMBL135328 25799 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@@H]1CN2CC[C@H]1C2 10.1021/jm9702903
10666533 11400 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
CHEMBL1180310 11400 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
CHEMBL121299 11400 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
10593954 13044 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.2 CCN1CC=C(c2ccccc2)C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1190178 13044 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.2 CCN1CC=C(c2ccccc2)C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL540316 13044 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.2 CCN1CC=C(c2ccccc2)C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
52947553 19076 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 374 3 0 4 3.4 O=C(c1ccoc1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289202 19076 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 374 3 0 4 3.4 O=C(c1ccoc1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
52943696 19233 3 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 348 3 0 2 4.2 O=C(c1ccccc1)N1CCC2(CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.10.016
CHEMBL1290294 19233 3 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 348 3 0 2 4.2 O=C(c1ccccc1)N1CCC2(CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.10.016
46890962 6988 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.4 O=C(Cc1ccccc1-c1cccc(Cl)c1)NC1CCNCC1 10.1016/j.bmcl.2010.04.127
CHEMBL1084804 6988 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.4 O=C(Cc1ccccc1-c1cccc(Cl)c1)NC1CCNCC1 10.1016/j.bmcl.2010.04.127
237 204842 48 None 1 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL546257 204842 48 None 1 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL554190 204842 48 None 1 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 204842 48 None 1 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
46891022 6630 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 380 4 2 2 4.5 O=C(NCC1CCNCC1)c1c(F)cccc1-c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2010.04.127
CHEMBL1083404 6630 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 380 4 2 2 4.5 O=C(NCC1CCNCC1)c1c(F)cccc1-c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2010.04.127
46871666 7037 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 342 4 2 2 4.0 CC1CNCCC1CNC(=O)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
CHEMBL1084993 7037 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 342 4 2 2 4.0 CC1CNCCC1CNC(=O)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
46891144 7239 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 364 4 2 2 4.0 O=C(NCC1(F)CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1085985 7239 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 364 4 2 2 4.0 O=C(NCC1(F)CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
656392 183776 3 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 255 5 1 4 1.4 CC[C@@H](C)[C@@H](O)C(=O)OC[C@H]1CCN2CCC[C@@H]12 10.1021/np049650x
CHEMBL480464 183776 3 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 255 5 1 4 1.4 CC[C@@H](C)[C@@H](O)C(=O)OC[C@H]1CCN2CCC[C@@H]12 10.1021/np049650x
44302879 202695 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 348 1 1 4 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL61774 202695 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 348 1 1 4 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3 10.1016/s0960-894x(98)00351-5
20735153 13591 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 nan
CHEMBL1194314 13591 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 nan
CHEMBL551063 13591 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 9 0 5 5.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 nan
44233177 13868 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 nan
CHEMBL1196246 13868 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 nan
CHEMBL556221 13868 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 7 0 4 5.7 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2Oc2ccccc21 nan
127053831 146198 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 7 0 3 6.1 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
CHEMBL3920279 146198 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 7 0 3 6.1 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
CHEMBL5285607 194281 0 None -1 5 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human muscarinic M3 receptor expressed in human HEK293T cells assessed as inhibition of carbachol-induced G-protein signaling by measuring inositol accumulation preincubated for 30 mins followed by carbachol stimulation and measured after 90 mins by HTRF assayBinding affinity to human muscarinic M3 receptor expressed in human HEK293T cells assessed as inhibition of carbachol-induced G-protein signaling by measuring inositol accumulation preincubated for 30 mins followed by carbachol stimulation and measured after 90 mins by HTRF assay
ChEMBL 1052 21 1 13 10.0 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
67547662 120859 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 482 7 2 3 4.2 CN(CCC[N+]12CCC(CC1)[C@@H](NC(=O)C1(O)c3ccccc3-c3ccccc31)C2)c1ccccc1 10.1016/j.bmcl.2015.02.065
CHEMBL3401653 120859 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 482 7 2 3 4.2 CN(CCC[N+]12CCC(CC1)[C@@H](NC(=O)C1(O)c3ccccc3-c3ccccc31)C2)c1ccccc1 10.1016/j.bmcl.2015.02.065
CHEMBL3559210 120859 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 482 7 2 3 4.2 CN(CCC[N+]12CCC(CC1)[C@@H](NC(=O)C1(O)c3ccccc3-c3ccccc31)C2)c1ccccc1 10.1016/j.bmcl.2015.02.065
154059 3610 51 None -1 8 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
2457 3610 51 None -1 8 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
7483 3610 51 None -1 8 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
CHEMBL1734 3610 51 None -1 8 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
DB01591 3610 51 None -1 8 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
44333603 109620 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 390 5 1 3 4.8 Cc1cc(C(=O)c2ccccc2)ccc1NC(=O)CC1CCCN2CCCC[C@H]12 10.1016/s0960-894x(99)00528-4
CHEMBL322378 109620 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 390 5 1 3 4.8 Cc1cc(C(=O)c2ccccc2)ccc1NC(=O)CC1CCCN2CCCC[C@H]12 10.1016/s0960-894x(99)00528-4
10567372 12099 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1160977 12099 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 12099 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333065 12099 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
44236332 13985 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
CHEMBL1197183 13985 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
CHEMBL561870 13985 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 7 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
127053830 149720 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 450 5 0 2 5.8 CC1(C(=O)O[C@H]2C[N+]3(C/C=C/c4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 nan
CHEMBL3948099 149720 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 450 5 0 2 5.8 CC1(C(=O)O[C@H]2C[N+]3(C/C=C/c4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 nan
127053828 149729 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 444 7 1 4 4.4 O=C(O[C@H]1C[N+]2(C/C=C/c3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccco1 nan
CHEMBL3948162 149729 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 444 7 1 4 4.4 O=C(O[C@H]1C[N+]2(C/C=C/c3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccco1 nan
135 2515 43 None -22 58 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2515 43 None -22 58 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2515 43 None -22 58 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2515 43 None -22 58 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2515 43 None -22 58 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
2774 3839 95 None -2 10 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
5593 3839 95 None -2 10 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
7319 3839 95 None -2 10 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
CHEMBL1200604 3839 95 None -2 10 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB00809 3839 95 None -2 10 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB01199 3839 95 None -2 10 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
10761219 11399 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.6 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1180309 11399 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.6 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL121298 11399 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.6 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
441383 20301 57 None -6 17 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 20301 57 None -6 17 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
12488 1644 56 None -8 23 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1644 56 None -8 23 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1644 56 None -8 23 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1644 56 None -8 23 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
44302741 202632 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 4 1 5 4.5 CCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL61412 202632 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 4 1 5 4.5 CCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
10569816 11427 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
CHEMBL1180367 11427 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
CHEMBL124173 11427 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
2750 204038 76 None -1 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 204038 76 None -1 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
2745 3832 42 None -21 9 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
5572 3832 42 None -21 9 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
66007 3832 42 None -21 9 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
7315 3832 42 None -21 9 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
CHEMBL1490 3832 42 None -21 9 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
DB00376 3832 42 None -21 9 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
118728610 117749 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 336 4 2 3 2.1 O=C(N[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2015.02.065
CHEMBL3401640 117749 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 336 4 2 3 2.1 O=C(N[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2015.02.065
9946632 62319 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 354 4 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)c1ccc(F)cc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779043 62319 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 354 4 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)c1ccc(F)cc1 10.1016/j.bmcl.2011.03.096
44232683 13594 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 nan
CHEMBL1194336 13594 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 nan
CHEMBL551731 13594 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 472 9 1 4 4.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 nan
52948443 19161 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 419 4 0 5 3.9 CCc1nc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289758 19161 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 419 4 0 5 3.9 CCc1nc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
52947254 19175 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 433 4 0 5 4.4 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289865 19175 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 433 4 0 5 4.4 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
13578554 172401 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 461 5 1 5 4.4 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCC1 10.1021/jm00128a008
CHEMBL44773 172401 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 461 5 1 5 4.4 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCC1 10.1021/jm00128a008
24750278 89395 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of M3 receptor (unknown origin)Inhibition of M3 receptor (unknown origin)
ChEMBL 450 6 1 9 1.7 CC(C)=CCn1c(N2CCC[C@H](N)C2)nc2c1c(=O)n(CC(=O)c1ccccc1)c(=O)n2C 10.1021/acs.jmedchem.6b00475
CHEMBL237067 89395 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of M3 receptor (unknown origin)Inhibition of M3 receptor (unknown origin)
ChEMBL 450 6 1 9 1.7 CC(C)=CCn1c(N2CCC[C@H](N)C2)nc2c1c(=O)n(CC(=O)c1ccccc1)c(=O)n2C 10.1021/acs.jmedchem.6b00475
13578554 172401 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 461 5 1 5 4.4 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCC1 10.1021/jm00048a014
CHEMBL44773 172401 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 461 5 1 5 4.4 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCC1 10.1021/jm00048a014
14075467 101453 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(Cl)ccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL297818 101453 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(Cl)ccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
13578552 160153 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 419 4 1 5 3.3 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCC2)c2ccccc21 10.1021/jm00128a008
CHEMBL410928 160153 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 419 4 1 5 3.3 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCC2)c2ccccc21 10.1021/jm00128a008
14590397 187673 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 407 5 1 5 3.1 CCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL49525 187673 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 407 5 1 5 3.1 CCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
13578555 176656 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity of compound for glandular Muscarinic acetylcholine receptor M3 in rat using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity of compound for glandular Muscarinic acetylcholine receptor M3 in rat using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 433 4 1 5 3.7 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCCC2)c2ccccc21 10.1021/jm00128a008
CHEMBL45983 176656 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity of compound for glandular Muscarinic acetylcholine receptor M3 in rat using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity of compound for glandular Muscarinic acetylcholine receptor M3 in rat using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 433 4 1 5 3.7 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCCC2)c2ccccc21 10.1021/jm00128a008
14075467 101453 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(Cl)ccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL297818 101453 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(Cl)ccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
13578552 160153 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 419 4 1 5 3.3 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCC2)c2ccccc21 10.1021/jm00048a014
CHEMBL410928 160153 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 419 4 1 5 3.3 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCC2)c2ccccc21 10.1021/jm00048a014
13578555 176656 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 433 4 1 5 3.7 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCCC2)c2ccccc21 10.1021/jm00048a014
CHEMBL45983 176656 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 433 4 1 5 3.7 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCCCC2)c2ccccc21 10.1021/jm00048a014
14590397 187673 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 407 5 1 5 3.1 CCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL49525 187673 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 407 5 1 5 3.1 CCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
14590396 172518 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 6 1 5 3.9 CCN(CC)CC1CCCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL44838 172518 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 6 1 5 3.9 CCN(CC)CC1CCCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
14590396 172518 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 6 1 5 3.9 CCN(CC)CC1CCCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL44838 172518 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 6 1 5 3.9 CCN(CC)CC1CCCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
2274 3151 58 None -21 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3151 58 None -21 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3151 58 None -21 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3151 58 None -21 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3151 58 None -21 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
44302901 101029 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 320 1 1 3 3.9 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)cc34)OC21 10.1016/s0960-894x(98)00351-5
CHEMBL294726 101029 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 320 1 1 3 3.9 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)cc34)OC21 10.1016/s0960-894x(98)00351-5
9905467 11404 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180316 11404 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL121520 11404 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
44190762 176856 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from muscarinic M3 receptorDisplacement of radioligand from muscarinic M3 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
CHEMBL461571 176856 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from muscarinic M3 receptorDisplacement of radioligand from muscarinic M3 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
4841 67397 5 None -3 5 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
CHEMBL1889399 67397 5 None -3 5 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
CHEMBL1909073 67397 5 None -3 5 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
52950036 19126 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 391 3 0 5 3.3 O=C(c1cscn1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289544 19126 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 391 3 0 5 3.3 O=C(c1cscn1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
57391772 69114 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 361 8 0 3 3.8 CCCN(CCC)C(C)(C(=O)OC1CC[N+](C)(C)CC1)c1ccccc1 10.1016/j.bmcl.2011.10.002
CHEMBL1924035 69114 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 361 8 0 3 3.8 CCCN(CCC)C(C)(C(=O)OC1CC[N+](C)(C)CC1)c1ccccc1 10.1016/j.bmcl.2011.10.002
127053832 150776 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 6 0 4 5.2 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
CHEMBL3956752 150776 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 6 0 4 5.2 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
66592494 151563 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 457 8 1 6 4.1 O=C(O[C@H]1C[N+]2(CCCn3cccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL3963421 151563 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 457 8 1 6 4.1 O=C(O[C@H]1C[N+]2(CCCn3cccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
10082470 52687 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 227 2 0 5 2.0 CSc1nsnc1C1=CCCN(C)C1 10.1021/jm9705216
CHEMBL15944 52687 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 227 2 0 5 2.0 CSc1nsnc1C1=CCCN(C)C1 10.1021/jm9705216
CHEMBL308608 52687 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 227 2 0 5 2.0 CSc1nsnc1C1=CCCN(C)C1 10.1021/jm9705216
10522336 15098 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.3 CCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL120972 15098 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.3 CCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
44302728 198690 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 422 4 1 6 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL58228 198690 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 422 4 1 6 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3 10.1016/s0960-894x(98)00351-5
10806268 12105 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.7 CCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1184139 12105 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.7 CCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL334245 12105 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 329 9 0 3 4.7 CCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
10664532 12080 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184064 12080 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL330892 12080 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 335 6 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
10518821 12095 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.6 CCN1CC=C(c2ccccc2)C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184108 12095 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.6 CCN1CC=C(c2ccccc2)C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
CHEMBL332645 12095 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.6 CCN1CC=C(c2ccccc2)C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
10611310 12091 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.7 CCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1184096 12091 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.7 CCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL332335 12091 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.7 CCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
9966959 62317 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 6 0 4 3.6 CCCCN(Cc1cccs1)C(=O)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
CHEMBL1779041 62317 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 6 0 4 3.6 CCCCN(Cc1cccs1)C(=O)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2011.03.096
11569926 63103 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 441 7 0 2 5.7 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779048 63103 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 441 7 0 2 5.7 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789434 63103 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 441 7 0 2 5.7 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)N(Cc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
2398 951 62 None -1 29 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 951 62 None -1 29 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 951 62 None -1 29 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 951 62 None -1 29 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 951 62 None -1 29 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
302 2956 25 None -309 8 Human 4.8 pIC50 = 4.8 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9705216
4630 2956 25 None -309 8 Human 4.8 pIC50 = 4.8 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9705216
CHEMBL7634 2956 25 None -309 8 Human 4.8 pIC50 = 4.8 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm9705216
1971 2846 38 None -4 30 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2846 38 None -4 30 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2846 38 None -4 30 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2846 38 None -4 30 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2846 38 None -4 30 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
67547652 117756 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 348 2 0 3 3.5 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.02.065
CHEMBL3401647 117756 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 348 2 0 3 3.5 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.02.065
4601 206724 35 None -1 17 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 206724 35 None -1 17 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 206724 35 None -1 17 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
28417 40009 49 None -1 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL1479 40009 49 None -1 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
191 402 98 None -37 29 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 402 98 None -37 29 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 402 98 None -37 29 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 402 98 None -37 29 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 402 98 None -37 29 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
3198 205490 76 None -10 34 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205490 76 None -10 34 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205490 76 None -10 34 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
43815 186896 64 None -5 25 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
CHEMBL1708 186896 64 None -5 25 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
CHEMBL490 186896 64 None -5 25 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
54586743 63111 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 357 4 0 3 4.1 C[N+]12CCC(CC1)[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2011.03.096
CHEMBL1779130 63111 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 357 4 0 3 4.1 C[N+]12CCC(CC1)[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2011.03.096
CHEMBL1789462 63111 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 357 4 0 3 4.1 C[N+]12CCC(CC1)[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2011.03.096
67549179 117754 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 2 2 3 2.1 O=C(N[C@H]1CN2CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1016/j.bmcl.2015.02.065
CHEMBL3401645 117754 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 2 2 3 2.1 O=C(N[C@H]1CN2CCC1CC2)C1(O)c2ccccc2-c2ccccc21 10.1016/j.bmcl.2015.02.065
10808719 12100 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184120 12100 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL333125 12100 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 363 8 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCc2ccccc2)C1 10.1021/jm980067l
448537 160226 89 None -28 25 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 160226 89 None -28 25 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
18456768 63105 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 407 8 0 2 5.3 CCCCN(C(=O)O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779134 63105 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 407 8 0 2 5.3 CCCCN(C(=O)O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1789445 63105 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 407 8 0 2 5.3 CCCCN(C(=O)O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
53372934 129274 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670826 129274 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
66592724 147918 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 476 6 1 5 4.9 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
CHEMBL3933797 147918 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 476 6 1 5 4.9 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
52942401 19186 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 433 4 0 5 4.4 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4ccccc4Cl)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289982 19186 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 433 4 0 5 4.4 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4ccccc4Cl)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
46891020 6628 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 363 5 1 3 4.2 O=S(=O)(CCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083402 6628 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 363 5 1 3 4.2 O=S(=O)(CCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
15730 71089 80 None -1 10 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
CHEMBL195437 71089 80 None -1 10 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
6075 150084 42 None -3 16 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 150084 42 None -3 16 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
10829928 12370 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.4 CCCCCc1noc(C2=C(c3ccccc3)CCN(CC)C2)n1 10.1021/jm980067l
CHEMBL1185758 12370 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.4 CCCCCc1noc(C2=C(c3ccccc3)CCN(CC)C2)n1 10.1021/jm980067l
CHEMBL431688 12370 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.4 CCCCCc1noc(C2=C(c3ccccc3)CCN(CC)C2)n1 10.1021/jm980067l
52946359 19091 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 3 0 6 2.7 O=C(c1cnsn1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289314 19091 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 3 0 6 2.7 O=C(c1cnsn1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
46890960 7155 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.6 O=C(NCc1ccccc1-c1cccc(Cl)c1)C1CCNCC1 10.1016/j.bmcl.2010.04.127
CHEMBL1085556 7155 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.6 O=C(NCc1ccccc1-c1cccc(Cl)c1)C1CCNCC1 10.1016/j.bmcl.2010.04.127
10053614 120854 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 483 9 2 5 4.2 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401651 120854 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 483 9 2 5 4.2 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559203 120854 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 483 9 2 5 4.2 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
54672859 148022 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 778 15 6 12 5.4 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(F)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3934681 148022 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 778 15 6 12 5.4 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(F)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
25897919 55622 14 None 1 8 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
657309 55622 14 None 1 8 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
CHEMBL1464005 55622 14 None 1 8 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
CHEMBL1621597 55622 14 None 1 8 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
174174 521 49 None -2 14 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
260 521 49 None -2 14 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
320 521 49 None -2 14 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
CHEMBL517712 521 49 None -2 14 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
DB00572 521 49 None -2 14 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
54675236 142684 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 808 15 6 12 6.3 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@](C)(OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3892218 142684 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 808 15 6 12 6.3 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@](C)(OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
53372938 129276 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670828 129276 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
11725334 117750 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 348 4 2 5 2.3 O=C(N[C@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401641 117750 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 348 4 2 5 2.3 O=C(N[C@H]1CN2CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
71559319 152478 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 760 16 6 12 4.4 CN(CCNC(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3971284 152478 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 760 16 6 12 4.4 CN(CCNC(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
54590927 149823 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 764 14 6 11 5.9 CN(CCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3948979 149823 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 764 14 6 11 5.9 CN(CCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
54585743 62320 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 372 4 0 3 4.2 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccc(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
CHEMBL1779044 62320 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 372 4 0 3 4.2 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccc(F)c1)c1cccc(F)c1 10.1016/j.bmcl.2011.03.096
57399405 68727 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 490 8 0 4 5.2 Cc1cc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cc(C)n1 10.1016/j.bmcl.2011.10.002
CHEMBL1921920 68727 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 490 8 0 4 5.2 Cc1cc(CCC[N+]23CCC(CC2)[C@@H](OC(=O)[C@](C)(c2ccccc2)N2CCCCC2)C3)cc(C)n1 10.1016/j.bmcl.2011.10.002
24988642 69116 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 379 4 0 3 3.8 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccc(Cl)cc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924037 69116 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 379 4 0 3 3.8 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccc(Cl)cc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72546737 103634 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccncc1 10.1016/j.bmcl.2013.09.092
CHEMBL3087365 103634 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccncc1 10.1016/j.bmcl.2013.09.092
72547253 103642 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 518 6 1 4 5.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2013.09.092
CHEMBL3087374 103642 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 518 6 1 4 5.4 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2013.09.092
72547499 103686 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 519 6 1 5 4.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(C(F)(F)F)nn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087945 103686 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 519 6 1 5 4.8 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccc(C(F)(F)F)nn1 10.1016/j.bmcl.2013.09.092
72545051 103704 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 3 0 2 4.0 C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2 10.1016/j.bmcl.2013.09.092
CHEMBL3088076 103704 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 330 3 0 2 4.0 C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2 10.1016/j.bmcl.2013.09.092
1734 116 10 None 1 13 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm701575k
307 116 10 None 1 13 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm701575k
CHEMBL168067 116 10 None 1 13 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm701575k
11852298 13994 0 None -1 3 Human 8.6 pIC50 = 8.6 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL1197251 13994 0 None -1 3 Human 8.6 pIC50 = 8.6 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL564057 13994 0 None -1 3 Human 8.6 pIC50 = 8.6 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
2028 2958 80 None 1 11 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
359 2958 80 None 1 11 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634 2958 80 None 1 11 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
CHEMBL1231 2958 80 None 1 11 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
DB01062 2958 80 None 1 11 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
53372938 129276 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670828 129276 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
2286 3161 51 None -1 30 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3161 51 None -1 30 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3161 51 None -1 30 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3161 51 None -1 30 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3161 51 None -1 30 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
14374296 101626 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 449 8 1 5 4.3 CCN(CC)CCCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL299142 101626 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 449 8 1 5 4.3 CCN(CC)CCCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
14590398 101839 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 7 1 5 3.9 CCCCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL300660 101839 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 7 1 5 3.9 CCCCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
44236338 13878 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 6 1 5 4.4 O=C(O[C@H]1C[N+]2(Cc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1196358 13878 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 6 1 5 4.4 O=C(O[C@H]1C[N+]2(Cc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL556634 13878 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 440 6 1 5 4.4 O=C(O[C@H]1C[N+]2(Cc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
14374296 101626 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 449 8 1 5 4.3 CCN(CC)CCCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL299142 101626 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 449 8 1 5 4.3 CCN(CC)CCCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
14590398 101839 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 7 1 5 3.9 CCCCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL300660 101839 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 7 1 5 3.9 CCCCN(C)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
14590402 101060 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(C)ccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL294919 101060 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(C)ccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
13578572 186875 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 407 6 1 5 3.1 CCN(CC)CC1CCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL48980 186875 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 407 6 1 5 3.1 CCN(CC)CC1CCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
14590403 188371 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 449 7 1 5 4.1 CCc1ccc2c(c1)C(=O)Nc1cccnc1N2C(=O)CN1CCCCC1CN(CC)CC 10.1021/jm00128a008
CHEMBL50176 188371 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 449 7 1 5 4.1 CCc1ccc2c(c1)C(=O)Nc1cccnc1N2C(=O)CN1CCCCC1CN(CC)CC 10.1021/jm00128a008
14590402 101060 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(C)ccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL294919 101060 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 6 1 5 3.8 CCN(CC)CC1CCCCN1CC(=O)N1c2cc(C)ccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
13578572 186875 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 407 6 1 5 3.1 CCN(CC)CC1CCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL48980 186875 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 407 6 1 5 3.1 CCN(CC)CC1CCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
14590403 188371 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 449 7 1 5 4.1 CCc1ccc2c(c1)C(=O)Nc1cccnc1N2C(=O)CN1CCCCC1CN(CC)CC 10.1021/jm00048a014
CHEMBL50176 188371 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 449 7 1 5 4.1 CCc1ccc2c(c1)C(=O)Nc1cccnc1N2C(=O)CN1CCCCC1CN(CC)CC 10.1021/jm00048a014
10546275 15170 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.5 CCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL121059 15170 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 357 11 0 3 5.5 CCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
10499832 12103 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.0 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184134 12103 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.0 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL334093 12103 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.0 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
2726 916 68 None -18 73 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 916 68 None -18 73 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 916 68 None -18 73 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 916 68 None -18 73 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 916 68 None -18 73 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
3500 1514 13 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 483 7 1 5 3.9 CCCCN1C(=O)C(CC2CCCCC2)NC(=O)C21CCN(CC2)Cc1ccc2c(c1)OCCO2 10.1021/jm060051s
491774 1514 13 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 483 7 1 5 3.9 CCCCN1C(=O)C(CC2CCCCC2)NC(=O)C21CCN(CC2)Cc1ccc2c(c1)OCCO2 10.1021/jm060051s
CHEMBL1196395 1514 13 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 483 7 1 5 3.9 CCCCN1C(=O)C(CC2CCCCC2)NC(=O)C21CCN(CC2)Cc1ccc2c(c1)OCCO2 10.1021/jm060051s
1548953 207656 27 None -2 17 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 207656 27 None -2 17 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
10591874 13284 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1192001 13284 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
CHEMBL543177 13284 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
66592813 150793 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 9 0 3 5.6 CC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)c1ccccc1 nan
CHEMBL3956822 150793 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 9 0 3 5.6 CC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)c1ccccc1 nan
54584800 62315 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 356 5 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)Cc1cccs1 10.1016/j.bmcl.2011.03.096
CHEMBL1779039 62315 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 356 5 0 4 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1ccccc1)Cc1cccs1 10.1016/j.bmcl.2011.03.096
10686988 12157 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 317 8 0 3 4.2 CCCCCCOC(=O)[C@H]1CN(CC)CC[C@H]1c1ccccc1 10.1021/jm980067l
CHEMBL1184244 12157 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 317 8 0 3 4.2 CCCCCCOC(=O)[C@H]1CN(CC)CC[C@H]1c1ccccc1 10.1021/jm980067l
CHEMBL340780 12157 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 317 8 0 3 4.2 CCCCCCOC(=O)[C@H]1CN(CC)CC[C@H]1c1ccccc1 10.1021/jm980067l
10678449 22621 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 154 2 0 3 0.6 CO/N=C/[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
CHEMBL132698 22621 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 154 2 0 3 0.6 CO/N=C/[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
1530 2169 50 None -57 21 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2169 50 None -57 21 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2169 50 None -57 21 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2169 50 None -57 21 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2169 50 None -57 21 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
44236334 13980 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 nan
CHEMBL1197117 13980 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 nan
CHEMBL559931 13980 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 468 7 0 3 5.6 CC1(C(=O)O[C@H]2C[N+]3(CCCOc4ccccc4)CCC2CC3)c2ccccc2-c2ccccc21 nan
10516408 11409 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180330 11409 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL122353 11409 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
3055 1421 44 None -1 9 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
313 1421 44 None -1 9 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
7163 1421 44 None -1 9 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
CHEMBL936 1421 44 None -1 9 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
DB01231 1421 44 None -1 9 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
10594386 11386 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180249 11386 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL118553 11386 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
72546492 103697 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 489 6 0 4 6.7 O=C(O[C@H]1C[N+]2(Cc3csc(-c4ccccc4)n3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3087956 103697 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 489 6 0 4 6.7 O=C(O[C@H]1C[N+]2(Cc3csc(-c4ccccc4)n3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
52942610 19295 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 384 3 0 3 3.8 O=C(c1ccccc1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1290635 19295 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 384 3 0 3 3.8 O=C(c1ccccc1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
57402223 69122 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 413 7 0 3 4.7 CCC(CC)[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
CHEMBL1924043 69122 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 413 7 0 3 4.7 CCC(CC)[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
46890977 6700 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2ccccc2C(=O)NCC2CCNCC2)cc1Cl 10.1016/j.bmcl.2010.04.128
CHEMBL1083723 6700 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2ccccc2C(=O)NCC2CCNCC2)cc1Cl 10.1016/j.bmcl.2010.04.128
46891075 6781 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083926 6781 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
10757736 14472 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL120135 14472 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
10755733 11396 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.4 CCN1CCC(c2ccccc2)=C(C(=O)OCC(C)C)C1 10.1021/jm980067l
CHEMBL1180297 11396 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.4 CCN1CCC(c2ccccc2)=C(C(=O)OCC(C)C)C1 10.1021/jm980067l
CHEMBL120581 11396 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.4 CCN1CCC(c2ccccc2)=C(C(=O)OCC(C)C)C1 10.1021/jm980067l
1210 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
1213 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
2725 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
33036 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
4411 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
616 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
6976 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
716121 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
90475904 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 915 51 None -79 21 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
180 400 56 None -23 40 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 400 56 None -23 40 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 400 56 None -23 40 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 400 56 None -23 40 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 400 56 None -23 40 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
5648 78382 9 None -1 5 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
CHEMBL2107687 78382 9 None -1 5 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
CHEMBL2111176 78382 9 None -1 5 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
2745 3832 42 None -21 9 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
5572 3832 42 None -21 9 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
66007 3832 42 None -21 9 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
7315 3832 42 None -21 9 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
CHEMBL1490 3832 42 None -21 9 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
DB00376 3832 42 None -21 9 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
44302775 202773 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 4 1 5 4.5 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OCC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL62247 202773 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 4 1 5 4.5 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OCC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
44302776 102323 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(C)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL303758 102323 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(C)ccc2C1O3 10.1016/s0960-894x(98)00351-5
10797864 26113 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB)radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB)radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 1.0 CO/N=C(\C#N)C12CCCN(CC1)C2 10.1021/jm9702903
CHEMBL135645 26113 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB)radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB)radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 1.0 CO/N=C(\C#N)C12CCCN(CC1)C2 10.1021/jm9702903
10522202 11402 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180312 11402 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL121385 11402 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
44302900 202775 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 3 1 5 4.5 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(C(=O)OC(C)C)c34)OC21 10.1016/s0960-894x(98)00351-5
CHEMBL62251 202775 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 406 3 1 5 4.5 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(C(=O)OC(C)C)c34)OC21 10.1016/s0960-894x(98)00351-5
44302833 102474 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(C)c2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL304036 102474 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(C)c2C1O3 10.1016/s0960-894x(98)00351-5
10755732 12089 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.4 CCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184092 12089 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.4 CCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL332181 12089 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.4 CCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
1016 3720 78 None -12 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3720 78 None -12 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3720 78 None -12 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3720 78 None -12 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3720 78 None -12 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3720 78 None -12 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
10567192 12064 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 3.9 CCN1CC=C(c2ccccc2)C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1183934 12064 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 3.9 CCN1CC=C(c2ccccc2)C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL324936 12064 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 3.9 CCN1CC=C(c2ccccc2)C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
657309 60198 14 None - 0 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1CC(OC(=O)C(CO)c1ccccc1)C2 nan
CHEMBL1740585 60198 14 None - 0 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1CC(OC(=O)C(CO)c1ccccc1)C2 nan
66591963 144223 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 460 7 1 6 4.5 O=C(O[C@H]1C[N+]2(CCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL3904721 144223 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 460 7 1 6 4.5 O=C(O[C@H]1C[N+]2(CCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
57400155 68657 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 448 7 0 4 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cccnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921802 68657 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 448 7 0 4 4.2 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cccnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397745 68730 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 463 8 0 5 4.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cncnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921923 68730 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 463 8 0 5 4.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCCc3cncnc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57397747 68737 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 481 8 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921930 68737 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 481 8 0 4 4.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccc(F)cc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
24988273 69107 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 331 4 0 3 2.8 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924028 69107 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 331 4 0 3 2.8 CC(C(=O)OC1CC[N+](C)(C)CC1)(c1ccccc1)N1CCCC1 10.1016/j.bmcl.2011.10.002
57397003 69120 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 5.0 C[C@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924041 69120 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 477 9 0 4 5.0 C[C@](C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72543917 103691 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 522 9 2 6 2.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)NCCNC(=O)c1cnccn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087950 103691 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 522 9 2 6 2.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)NCCNC(=O)c1cnccn1 10.1016/j.bmcl.2013.09.092
72545280 103707 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 436 6 0 3 5.6 COc1cccc(C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c1 10.1016/j.bmcl.2013.09.092
CHEMBL3088079 103707 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 436 6 0 3 5.6 COc1cccc(C[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)c1 10.1016/j.bmcl.2013.09.092
72545284 103710 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 445 6 0 3 5.5 N#Cc1ccc(CC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cc1 10.1016/j.bmcl.2013.09.092
CHEMBL3088083 103710 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 445 6 0 3 5.5 N#Cc1ccc(CC[N+]23CCC(CC2)[C@@H](OC(=O)C2(C4=CC=CC4)CCCCCC2)C3)cc1 10.1016/j.bmcl.2013.09.092
174174 521 49 None -2 14 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
260 521 49 None -2 14 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
320 521 49 None -2 14 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
CHEMBL517712 521 49 None -2 14 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
DB00572 521 49 None -2 14 Human 8.5 pIC50 = 8.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
10132599 62308 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 350 5 0 3 4.0 O=C(O[C@H]1CN2CCC1CC2)N(CCc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779032 62308 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 350 5 0 3 4.0 O=C(O[C@H]1CN2CCC1CC2)N(CCc1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
71566170 144889 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 17 7 12 4.5 CC(Cc1ccc(OCC(=O)NCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3910208 144889 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 774 17 7 12 4.5 CC(Cc1ccc(OCC(=O)NCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
71278078 144465 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 796 15 6 12 6.2 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)[C@](O)(c3cccs3)C3CCCC3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3906808 144465 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 796 15 6 12 6.2 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)[C@](O)(c3cccs3)C3CCCC3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
44236340 13760 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL1195513 13760 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL554725 13760 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 482 9 1 5 5.2 O=C(O[C@H]1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
52945272 19176 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 399 4 0 5 3.8 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4ccccc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289866 19176 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 399 4 0 5 3.8 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4ccccc4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
13578571 101097 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)C1 10.1021/jm00128a008
CHEMBL295214 101097 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)C1 10.1021/jm00128a008
CHEMBL5271406 193657 0 None -3 5 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human muscarinic M3 receptor expressed in human HEK293T cells assessed as inhibition of carbachol-induced G-protein signaling by measuring inositol accumulation preincubated for 30 mins followed by carbachol stimulation and measured after 90 mins by HTRF assayBinding affinity to human muscarinic M3 receptor expressed in human HEK293T cells assessed as inhibition of carbachol-induced G-protein signaling by measuring inositol accumulation preincubated for 30 mins followed by carbachol stimulation and measured after 90 mins by HTRF assay
ChEMBL 1159 27 3 10 12.8 CC1(C)C(/C=C/C=C/C=C2/N(CCCCS(=O)(=O)O)c3ccccc3C2(C)C)=[N+](CCCCCC(=O)NCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(F)c(Cl)c3)CC2)c2ccc(S(=O)(=O)[O-])cc21 10.1021/acs.jmedchem.2c01376
25070582 61424 28 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 61424 28 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
2200 3109 46 None -11 13 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/s0960-894x(99)00528-4
328 3109 46 None -11 13 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/s0960-894x(99)00528-4
4848 3109 46 None -11 13 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/s0960-894x(99)00528-4
CHEMBL9967 3109 46 None -11 13 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/s0960-894x(99)00528-4
DB00670 3109 46 None -11 13 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/s0960-894x(99)00528-4
10726038 119406 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 179 2 0 4 0.6 CO/N=C(\C#N)C12CCN(CC1)C2 10.1021/jm9702903
CHEMBL344892 119406 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 179 2 0 4 0.6 CO/N=C(\C#N)C12CCN(CC1)C2 10.1021/jm9702903
13578571 101097 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)C1 10.1021/jm00048a014
CHEMBL295214 101097 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)C1 10.1021/jm00048a014
14590399 101251 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 393 5 2 5 2.8 CCNCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL296365 101251 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 393 5 2 5 2.8 CCNCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
24739387 188133 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 454 4 0 2 5.2 CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
CHEMBL498556 188133 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 454 4 0 2 5.2 CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 10.1016/j.bmcl.2008.07.115
14590399 101251 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 393 5 2 5 2.8 CCNCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL296365 101251 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 393 5 2 5 2.8 CCNCC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
44302834 202687 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 454 4 1 5 5.9 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Oc4ccccc4)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL61700 202687 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 454 4 1 5 5.9 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Oc4ccccc4)ccc2C1O3 10.1016/s0960-894x(98)00351-5
127053829 145400 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 452 5 1 3 4.8 O=C(O[C@H]1C[N+]2(C/C=C/c3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
CHEMBL3914137 145400 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 452 5 1 3 4.8 O=C(O[C@H]1C[N+]2(C/C=C/c3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
69994004 154133 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 9 0 3 5.8 O=C(O[C@@H]1CC2CC[N+]1(CCCOc1ccccc1)CC2)C(c1ccccc1)c1ccccc1 nan
CHEMBL3985491 154133 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 9 0 3 5.8 O=C(O[C@@H]1CC2CC[N+]1(CCCOc1ccccc1)CC2)C(c1ccccc1)c1ccccc1 nan
87064156 160211 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 458 4 1 4 4.8 CCC1([N+]23CCC(CC2)[C@@H](OC(=O)C2(O)c4ccccc4-c4ccccc42)C3)c2ccsc21 nan
CHEMBL4109862 160211 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 458 4 1 4 4.8 CCC1([N+]23CCC(CC2)[C@@H](OC(=O)C2(O)c4ccccc4-c4ccccc42)C3)c2ccsc21 nan
52949961 19316 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 424 3 0 4 4.6 O=C(c1ccc2occc2c1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1290752 19316 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 424 3 0 4 4.6 O=C(c1ccc2occc2c1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
72546735 103632 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087363 103632 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 450 6 1 4 4.4 O=C(C[N+]12CCC(CC1)[C@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1ccccn1 10.1016/j.bmcl.2013.09.092
11318734 187306 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human cloned muscarinic M3 receptor expressed in CHO cells by FLIPR assayInhibition of human cloned muscarinic M3 receptor expressed in CHO cells by FLIPR assay
ChEMBL 429 6 2 5 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1021/jm800935u
CHEMBL493079 187306 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human cloned muscarinic M3 receptor expressed in CHO cells by FLIPR assayInhibition of human cloned muscarinic M3 receptor expressed in CHO cells by FLIPR assay
ChEMBL 429 6 2 5 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1021/jm800935u
4746 204868 31 None -1 4 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL1334033 204868 31 None -1 4 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL75880 204868 31 None -1 4 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
10759393 84356 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL2112589 84356 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL2219563 84356 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
4189 206899 96 None -12 34 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206899 96 None -12 34 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206899 96 None -12 34 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
52943721 19257 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 354 3 0 3 4.3 O=C(c1ccsc1)N1CCC2(CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.10.016
CHEMBL1290410 19257 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 354 3 0 3 4.3 O=C(c1ccsc1)N1CCC2(CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.10.016
46891076 6676 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 344 4 2 2 3.8 O=C(NCC1=CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083618 6676 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 344 4 2 2 3.8 O=C(NCC1=CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
10688349 12104 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184138 12104 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL334194 12104 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1 10.1021/jm980067l
176 397 66 None -1 31 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 397 66 None -1 31 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 397 66 None -1 31 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 397 66 None -1 31 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 397 66 None -1 31 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
44302793 199706 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 350 2 1 4 3.9 COc1cc2c(cc1OC)C1Oc3ccc4[nH]c(C)cc4c3CN1CC2 10.1016/s0960-894x(98)00351-5
CHEMBL59347 199706 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 350 2 1 4 3.9 COc1cc2c(cc1OC)C1Oc3ccc4[nH]c(C)cc4c3CN1CC2 10.1016/s0960-894x(98)00351-5
10392705 120855 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 9 1 4 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401652 120855 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 9 1 4 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559204 120855 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 467 9 1 4 5.1 O=C(N[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
9882189 167410 33 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to muscarinic 3 receptor (unknown origin)Binding affinity to muscarinic 3 receptor (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1016/j.bmc.2022.117032
CHEMBL4297224 167410 33 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to muscarinic 3 receptor (unknown origin)Binding affinity to muscarinic 3 receptor (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1016/j.bmc.2022.117032
9882189 167410 33 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to muscarinic acetylcholine receptor M3 (unknown origin)Binding affinity to muscarinic acetylcholine receptor M3 (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01192
CHEMBL4297224 167410 33 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to muscarinic acetylcholine receptor M3 (unknown origin)Binding affinity to muscarinic acetylcholine receptor M3 (unknown origin)
ChEMBL 281 4 0 2 3.5 CN(C)CC1CCOC1(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01192
324 1912 15 None -17 9 Human 6.5 pIC50 = 6.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(98)00351-5
6436265 1912 15 None -17 9 Human 6.5 pIC50 = 6.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(98)00351-5
CHEMBL277642 1912 15 None -17 9 Human 6.5 pIC50 = 6.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(98)00351-5
44302788 200599 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 378 2 1 5 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL59939 200599 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 378 2 1 5 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
2683 102861 25 None 1 16 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102861 25 None 1 16 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102861 25 None 1 16 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
5318 15544 49 None -1 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 15544 49 None -1 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 15544 49 None -1 13 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
10358345 11410 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.3 CCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1180331 11410 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.3 CCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL122354 11410 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.3 CCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
71454411 78420 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 390 2 1 4 4.0 O=C1Nc2cccnc2N(C(=O)C[C@H]2CCCN3CCCCC23)c2ccccc21 10.1016/s0960-894x(99)00528-4
CHEMBL2111621 78420 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 390 2 1 4 4.0 O=C1Nc2cccnc2N(C(=O)C[C@H]2CCCN3CCCCC23)c2ccccc21 10.1016/s0960-894x(99)00528-4
10851853 12156 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.9 CCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1184242 12156 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.9 CCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL340561 12156 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.9 CCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
1209 1645 75 None -30 32 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
203 1645 75 None -30 32 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
3386 1645 75 None -30 32 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
CHEMBL41 1645 75 None -30 32 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
DB00472 1645 75 None -30 32 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
53372936 129275 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670827 129275 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
11695697 117755 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 2 1 3 3.1 O=C(N[C@H]1CN2CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2015.02.065
CHEMBL3401646 117755 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 334 2 1 3 3.1 O=C(N[C@H]1CN2CCC1CC2)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2015.02.065
5310989 200854 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 378 3 1 5 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL60142 200854 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 378 3 1 5 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1016/s0960-894x(98)00351-5
10487582 28198 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
CHEMBL137384 28198 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 179 2 0 4 0.5 CO/N=C(\C#N)[C@H]1CN2CC[C@H]1C2 10.1021/jm9702903
2335 11816 22 None -1 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
8478 11816 22 None -1 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL1182210 11816 22 None -1 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL221753 11816 22 None -1 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
26987 946 33 None -56 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 946 33 None -56 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 946 33 None -56 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 946 33 None -56 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 946 33 None -56 21 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
72545052 103705 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 406 5 0 2 5.6 O=C(O[C@H]1C[N+]2(Cc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088077 103705 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 406 5 0 2 5.6 O=C(O[C@H]1C[N+]2(Cc3ccccc3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
72545053 103706 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 442 5 0 2 5.8 O=C(O[C@H]1C[N+]2(Cc3ccc(F)c(F)c3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
CHEMBL3088078 103706 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 442 5 0 2 5.8 O=C(O[C@H]1C[N+]2(Cc3ccc(F)c(F)c3)CCC1CC2)C1(C2=CC=CC2)CCCCCC1 10.1016/j.bmcl.2013.09.092
46871844 6780 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083925 6780 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
135398745 2893 112 None -27 66 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2893 112 None -27 66 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2893 112 None -27 66 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2893 112 None -27 66 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
52943921 19092 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 386 3 0 5 2.6 O=C(c1ncccn1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289315 19092 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 386 3 0 5 2.6 O=C(c1ncccn1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
52945165 19109 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 375 3 0 5 2.8 O=C(c1ccon1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289432 19109 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 375 3 0 5 2.8 O=C(c1ccon1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
52946068 19201 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 413 4 0 5 4.1 Cc1ccccc1CN1CCC2(CC1)CN(C(=O)c1csc(C(C)C)n1)CCO2 10.1016/j.bmcl.2010.10.016
CHEMBL1290077 19201 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 413 4 0 5 4.1 Cc1ccccc1CN1CCC2(CC1)CN(C(=O)c1csc(C(C)C)n1)CCO2 10.1016/j.bmcl.2010.10.016
46891021 6629 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 391 3 1 4 5.3 Fc1cccc(-c2cc(Cl)ccc2Cl)c1-c1nc(C2CCNCC2)no1 10.1016/j.bmcl.2010.04.127
CHEMBL1083403 6629 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 391 3 1 4 5.3 Fc1cccc(-c2cc(Cl)ccc2Cl)c1-c1nc(C2CCNCC2)no1 10.1016/j.bmcl.2010.04.127
46891488 7141 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.7 O=C(NCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
CHEMBL1085507 7141 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 328 4 2 2 3.7 O=C(NCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
10785471 113689 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.9 CCCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL332320 113689 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.9 CCCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
9857572 62312 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 302 5 0 3 3.5 CCCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779036 62312 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 302 5 0 3 3.5 CCCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
3042 1402 35 None -1 15 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1402 35 None -1 15 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1402 35 None -1 15 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1402 35 None -1 15 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1402 35 None -1 15 Human 8.4 pIC50 = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
11434515 261 6 None -4 5 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 nan
11519741 261 6 None -4 5 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 nan
4484 261 6 None -4 5 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 nan
7449 261 6 None -4 5 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 nan
CHEMBL1194325 261 6 None -4 5 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 nan
DB08897 261 6 None -4 5 Human 8.4 pIC50 = 8.4 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 nan
66592531 152828 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1cccs1 nan
CHEMBL3974189 152828 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 478 9 1 5 4.6 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1cccs1 nan
10267601 12097 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1184116 12097 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL332980 12097 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 313 4 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OC2CCCCC2)C1 10.1021/jm980067l
14590395 101491 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00128a008
CHEMBL298078 101491 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00128a008
379653 101656 2 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 499 6 1 5 4.3 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Br)cc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL299344 101656 2 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 499 6 1 5 4.3 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Br)cc2C(=O)Nc2cccnc21 10.1021/jm00128a008
13578553 168095 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 4 1 6 2.5 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCOCC2)c2ccccc21 10.1021/jm00128a008
CHEMBL432886 168095 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 4 1 6 2.5 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCOCC2)c2ccccc21 10.1021/jm00128a008
14590401 187954 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Cl)cc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL49721 187954 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Cl)cc2C(=O)Nc2cccnc21 10.1021/jm00128a008
14590395 101491 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00048a014
CHEMBL298078 101491 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.4 CCN(CC)CC1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00048a014
379653 101656 2 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 499 6 1 5 4.3 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Br)cc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL299344 101656 2 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 499 6 1 5 4.3 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Br)cc2C(=O)Nc2cccnc21 10.1021/jm00048a014
13578553 168095 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 4 1 6 2.5 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCOCC2)c2ccccc21 10.1021/jm00048a014
CHEMBL432886 168095 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 4 1 6 2.5 O=C1Nc2cccnc2N(C(=O)CN2CCCCC2CN2CCOCC2)c2ccccc21 10.1021/jm00048a014
14590401 187954 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Cl)cc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL49721 187954 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 455 6 1 5 4.2 CCN(CC)CC1CCCCN1CC(=O)N1c2ccc(Cl)cc2C(=O)Nc2cccnc21 10.1021/jm00048a014
10663572 13127 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1190784 13127 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
CHEMBL541584 13127 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 321 5 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCc2ccccc2)C1 10.1021/jm980067l
10614695 12125 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.8 CCN1CCC(c2ccccc2)=C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184188 12125 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.8 CCN1CCC(c2ccccc2)=C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
CHEMBL338280 12125 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 307 4 0 3 3.8 CCN1CCC(c2ccccc2)=C(C(=O)Oc2ccccc2)C1 10.1021/jm980067l
2284 3160 33 None -10 29 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3160 33 None -10 29 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3160 33 None -10 29 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3160 33 None -10 29 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3160 33 None -10 29 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL5285607 194281 0 None -1 5 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin recruitment preincubated for 30 mins followed by carbachol stimulation and measured after 90 mins by PathHunter assayBinding affinity to human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin recruitment preincubated for 30 mins followed by carbachol stimulation and measured after 90 mins by PathHunter assay
ChEMBL 1052 21 1 13 10.0 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
11057 176125 23 None -2 20 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
3468 176125 23 None -2 20 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 176125 23 None -2 20 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL64894 176125 23 None -2 20 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
124087 1377 114 None -9 15 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1377 114 None -9 15 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1377 114 None -9 15 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1377 114 None -9 15 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1377 114 None -9 15 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
10660 14384 58 None -2 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
CHEMBL1200406 14384 58 None -2 12 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
11793999 12083 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1184074 12083 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL331516 12083 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 377 9 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL5271406 193657 0 None -3 5 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin recruitment preincubated for 30 mins followed by carbachol stimulation and measured after 90 mins by PathHunter assayBinding affinity to human muscarinic M3 receptor expressed in human HEK293T cells cells co-expressing beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin recruitment preincubated for 30 mins followed by carbachol stimulation and measured after 90 mins by PathHunter assay
ChEMBL 1159 27 3 10 12.8 CC1(C)C(/C=C/C=C/C=C2/N(CCCCS(=O)(=O)O)c3ccccc3C2(C)C)=[N+](CCCCCC(=O)NCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(F)c(Cl)c3)CC2)c2ccc(S(=O)(=O)[O-])cc21 10.1021/acs.jmedchem.2c01376
25014630 83510 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1 10.1016/j.ejmech.2012.07.006
CHEMBL2203713 83510 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1 10.1016/j.ejmech.2012.07.006
10852843 11892 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1182713 11892 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
CHEMBL262303 11892 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1 10.1021/jm980067l
5353853 17954 47 None -13 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 17954 47 None -13 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 17954 47 None -13 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
135466875 189091 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 769 25 5 10 6.6 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
CHEMBL510340 189091 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 769 25 5 10 6.6 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
10567372 12099 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1160977 12099 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 12099 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333065 12099 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
277 1289 62 None -11 46 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1289 62 None -11 46 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1289 62 None -11 46 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1289 62 None -11 46 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1289 62 None -11 46 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
657255 199061 34 None -11 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 199061 34 None -11 15 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
3013847 188891 1 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 741 23 5 10 5.8 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
CHEMBL507760 188891 1 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 741 23 5 10 5.8 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
1212 1649 50 None -407 66 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1649 50 None -407 66 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1649 50 None -407 66 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1649 50 None -407 66 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1649 50 None -407 66 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
4011 82379 49 None -14 24 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 82379 49 None -14 24 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
66592626 151777 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 474 8 1 6 4.9 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL3965159 151777 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 474 8 1 6 4.9 O=C(O[C@H]1C[N+]2(CCCc3cccs3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
52942402 19187 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 433 4 0 5 4.4 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4cccc(Cl)c4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289983 19187 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 433 4 0 5 4.4 CC(C)c1nc(C(=O)N2CCOC3(CCN(Cc4cccc(Cl)c4)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
57392514 68741 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 464 8 0 5 4.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccncc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921934 68741 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 464 8 0 5 4.0 C[C@@](C(=O)O[C@H]1C[N+]2(CCOc3ccncc3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
57400423 69117 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 316 4 0 4 2.6 CN1CCC(OC(=O)C(C)(c2ccccc2)N2CCCC2)CC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924038 69117 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 316 4 0 4 2.6 CN1CCC(OC(=O)C(C)(c2ccccc2)N2CCCC2)CC1 10.1016/j.bmcl.2011.10.002
57393501 69118 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 328 4 0 4 2.6 CC(C(=O)O[C@H]1CN2CCC1CC2)(c1ccccc1)N1CCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924039 69118 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 328 4 0 4 2.6 CC(C(=O)O[C@H]1CN2CCC1CC2)(c1ccccc1)N1CCCC1 10.1016/j.bmcl.2011.10.002
57403965 69123 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 399 7 0 3 4.3 CCCC[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
CHEMBL1924044 69123 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 399 7 0 3 4.3 CCCC[N+]12CCC(CC1)[C@@H](OC(=O)[C@](C)(c1ccccc1)N1CCCCC1)C2 10.1016/j.bmcl.2011.10.002
1734 116 10 None 1 13 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmcl.2013.01.025
307 116 10 None 1 13 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL168067 116 10 None 1 13 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmcl.2013.01.025
44233401 13592 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 nan
CHEMBL1194321 13592 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 nan
CHEMBL551327 13592 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccsc1)c1ccsc1 nan
66592194 150564 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 502 9 1 6 4.8 O=C(O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL3955111 150564 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 502 9 1 6 4.8 O=C(O[C@H]1C[N+]2(CCCOc3ccc(F)cc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
10133281 62316 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 5 0 5 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccs1)Cc1cccs1 10.1016/j.bmcl.2011.03.096
CHEMBL1779040 62316 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 362 5 0 5 4.0 O=C(O[C@H]1CN2CCC1CC2)N(Cc1cccs1)Cc1cccs1 10.1016/j.bmcl.2011.03.096
122238756 147003 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 734 14 5 10 6.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c(NC=O)c3)ccc21)[C@H]1CC[C@H](c2cccc3c2C(C)(C(=O)O)c2ccccc2O3)CC1 nan
CHEMBL3926721 147003 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 ul. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 uM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 ug/well, respectively. After an incubation period of two hours with gentle shaking, 150 ul of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer.
ChEMBL 734 14 5 10 6.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c(NC=O)c3)ccc21)[C@H]1CC[C@H](c2cccc3c2C(C)(C(=O)O)c2ccccc2O3)CC1 nan
52943879 19317 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 388 3 0 4 3.7 Cc1ccc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)o1 10.1016/j.bmcl.2010.10.016
CHEMBL1290753 19317 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 388 3 0 4 3.7 Cc1ccc(C(=O)N2CCOC3(CCN(Cc4ccc(Cl)cc4)CC3)C2)o1 10.1016/j.bmcl.2010.10.016
46891179 6385 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 378 4 2 2 4.2 C[C@H]1CNCC[C@]1(F)CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1082365 6385 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human muscarinic M3 receptor expressed in CHO cellsInhibition of human muscarinic M3 receptor expressed in CHO cells
ChEMBL 378 4 2 2 4.2 C[C@H]1CNCC[C@]1(F)CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
10573693 11398 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.5 CCN1CCC(c2ccccc2)=C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
CHEMBL1180305 11398 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.5 CCN1CCC(c2ccccc2)=C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
CHEMBL120963 11398 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.5 CCN1CCC(c2ccccc2)=C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
10567372 12099 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1160977 12099 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 12099 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333065 12099 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
10595006 11413 0 None -8 5 Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
CHEMBL1180343 11413 0 None -8 5 Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
CHEMBL123099 11413 0 None -8 5 Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm980067l
10595006 11413 0 None -8 5 Human 4.3 pIC50 = 4.3 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
CHEMBL1180343 11413 0 None -8 5 Human 4.3 pIC50 = 4.3 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
CHEMBL123099 11413 0 None -8 5 Human 4.3 pIC50 = 4.3 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
10521205 11397 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.5 CCN1CC=C(c2ccccc2)C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180298 11397 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.5 CCN1CC=C(c2ccccc2)C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL120599 11397 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 341 6 0 3 4.5 CCN1CC=C(c2ccccc2)C(C(=O)OCCC2CCCCC2)C1 10.1021/jm980067l
10684720 12062 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.5 CCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1183926 12062 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.5 CCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL324712 12062 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 6 0 3 3.5 CCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
44356367 118466 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 266 3 0 2 2.2 C[N+](C)(C)CC#CCOC(=O)c1cccc(Cl)c1 10.1021/jm9702903
CHEMBL341447 118466 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 266 3 0 2 2.2 C[N+](C)(C)CC#CCOC(=O)c1cccc(Cl)c1 10.1021/jm9702903
44302813 101903 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 362 2 1 4 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3 10.1016/s0960-894x(98)00351-5
CHEMBL301041 101903 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 362 2 1 4 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3 10.1016/s0960-894x(98)00351-5
10610375 11390 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm980067l
CHEMBL1180284 11390 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm980067l
CHEMBL120109 11390 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm980067l
10610375 11390 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm301774u
CHEMBL1180284 11390 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm301774u
CHEMBL120109 11390 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1 10.1021/jm301774u
49853884 90654 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity to M3 receptor (unknown origin) by radioligand displacement assayBinding affinity to M3 receptor (unknown origin) by radioligand displacement assay
ChEMBL 265 3 1 3 1.2 O=C(CN1CCN2CCC[C@H]2C1)NC1CCCCC1 10.1016/j.bmc.2013.02.058
CHEMBL2391353 90654 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity to M3 receptor (unknown origin) by radioligand displacement assayBinding affinity to M3 receptor (unknown origin) by radioligand displacement assay
ChEMBL 265 3 1 3 1.2 O=C(CN1CCN2CCC[C@H]2C1)NC1CCCCC1 10.1016/j.bmc.2013.02.058
2230 464 60 None -588 10 Human 4.2 pIC50 = 4.2 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
296 464 60 None -588 10 Human 4.2 pIC50 = 4.2 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
CHEMBL7303 464 60 None -588 10 Human 4.2 pIC50 = 4.2 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
DB04365 464 60 None -588 10 Human 4.2 pIC50 = 4.2 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705216
3013845 188725 1 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 729 21 5 11 5.1 CCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL505197 188725 1 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 729 21 5 11 5.1 CCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
10460514 120857 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 483 9 2 5 4.2 O=C(N[C@@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401658 120857 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 483 9 2 5 4.2 O=C(N[C@@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3559206 120857 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 483 9 2 5 4.2 O=C(N[C@@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1016/j.bmcl.2015.02.065
9798900 63106 1 None - 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 3 1 3 4.1 O=C(Nc1ccccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmcl.2011.03.096
CHEMBL1779047 63106 1 None - 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 3 1 3 4.1 O=C(Nc1ccccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmcl.2011.03.096
CHEMBL1789446 63106 1 None - 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 3 1 3 4.1 O=C(Nc1ccccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmcl.2011.03.096
11569908 13969 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
CHEMBL1197028 13969 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
CHEMBL559106 13969 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 440 5 0 3 5.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
57397742 68721 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 487 7 0 4 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cc4ccccc4o3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1921912 68721 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 487 7 0 4 5.5 C[C@@](C(=O)O[C@H]1C[N+]2(CCc3cc4ccccc4o3)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
72543918 103692 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 535 10 2 5 3.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)NCCCNC(=O)c1ccccn1 10.1016/j.bmcl.2013.09.092
CHEMBL3087951 103692 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 535 10 2 5 3.7 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)NCCCNC(=O)c1ccccn1 10.1016/j.bmcl.2013.09.092
66592271 149930 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 448 8 1 5 3.7 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccco1 nan
CHEMBL3949833 149930 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 448 8 1 5 3.7 O=C(O[C@H]1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccco1 nan
66592394 153381 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 462 9 1 5 4.1 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccco1 nan
CHEMBL3978891 153381 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 462 9 1 5 4.1 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccco1 nan
44236101 13996 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
CHEMBL1197261 13996 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
CHEMBL564515 13996 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 456 5 1 4 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2Oc2ccccc21 nan
306 3430 21 None -4 5 Human 7.2 pIC50 = 7.2 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
3536 3430 21 None -4 5 Human 7.2 pIC50 = 7.2 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
53930639 3430 21 None -4 5 Human 7.2 pIC50 = 7.2 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
9577995 3430 21 None -4 5 Human 7.2 pIC50 = 7.2 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
CHEMBL134641 3430 21 None -4 5 Human 7.2 pIC50 = 7.2 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1021/jm9702903
67548544 120856 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 559 8 0 3 7.1 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1C[N+]2(CCCOc3ccc(-c4ccccc4)cc3)CCC1CC2 10.1016/j.bmcl.2015.02.065
CHEMBL3401656 120856 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 559 8 0 3 7.1 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1C[N+]2(CCCOc3ccc(-c4ccccc4)cc3)CCC1CC2 10.1016/j.bmcl.2015.02.065
CHEMBL3559205 120856 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 559 8 0 3 7.1 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1C[N+]2(CCCOc3ccc(-c4ccccc4)cc3)CCC1CC2 10.1016/j.bmcl.2015.02.065
2200 3109 46 None -11 13 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00128a008
328 3109 46 None -11 13 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00128a008
4848 3109 46 None -11 13 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00128a008
CHEMBL9967 3109 46 None -11 13 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00128a008
DB00670 3109 46 None -11 13 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00128a008
13578549 101247 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 7 1 5 3.9 CCN(CC)CC1CCCCN1CCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL296317 101247 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 435 7 1 5 3.9 CCN(CC)CC1CCCCN1CCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
13578549 101247 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 7 1 5 3.9 CCN(CC)CC1CCCCN1CCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL296317 101247 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 435 7 1 5 3.9 CCN(CC)CC1CCCCN1CCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
107867 2953 55 None -12 11 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00128a008
309 2953 55 None -12 11 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00128a008
CHEMBL17045 2953 55 None -12 11 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00128a008
14590400 177438 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 449 8 1 5 4.3 CCCN(CCC)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
CHEMBL46390 177438 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 449 8 1 5 4.3 CCCN(CCC)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00128a008
107867 2953 55 None -12 11 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00048a014
309 2953 55 None -12 11 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00048a014
CHEMBL17045 2953 55 None -12 11 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00048a014
14590400 177438 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 449 8 1 5 4.3 CCCN(CCC)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL46390 177438 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 449 8 1 5 4.3 CCCN(CCC)CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00048a014
CHEMBL1200633 208577 3 None -4 8 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL None None None CC[C@H](C)[C@H]1O[C@]2(CC[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(CC[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O nan
13583409 11423 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Compound was tested in vitro for its ability to displace [3H]QNB from brain Muscarinic acetylcholine receptor by 50 %Compound was tested in vitro for its ability to displace [3H]QNB from brain Muscarinic acetylcholine receptor by 50 %
ChEMBL 128 3 1 1 -0.0 OCC[N+]1(C2CC2)CC1 10.1021/jm00153a012
CHEMBL1180358 11423 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Compound was tested in vitro for its ability to displace [3H]QNB from brain Muscarinic acetylcholine receptor by 50 %Compound was tested in vitro for its ability to displace [3H]QNB from brain Muscarinic acetylcholine receptor by 50 %
ChEMBL 128 3 1 1 -0.0 OCC[N+]1(C2CC2)CC1 10.1021/jm00153a012
CHEMBL123573 11423 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Compound was tested in vitro for its ability to displace [3H]QNB from brain Muscarinic acetylcholine receptor by 50 %Compound was tested in vitro for its ability to displace [3H]QNB from brain Muscarinic acetylcholine receptor by 50 %
ChEMBL 128 3 1 1 -0.0 OCC[N+]1(C2CC2)CC1 10.1021/jm00153a012
135423423 188982 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 813 27 5 11 7.5 CCCCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL508807 188982 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 813 27 5 11 7.5 CCCCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
52942628 19055 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 374 3 0 4 3.4 O=C(c1ccco1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289081 19055 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 374 3 0 4 3.4 O=C(c1ccco1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
52946249 19056 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 390 3 0 4 3.9 O=C(c1cccs1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
CHEMBL1289082 19056 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 390 3 0 4 3.9 O=C(c1cccs1)N1CCOC2(CCN(Cc3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.10.016
3013846 188215 2 None 1 5 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 757 23 5 11 5.9 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL499519 188215 2 None 1 5 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 757 23 5 11 5.9 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
10567372 12099 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1160977 12099 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1184119 12099 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333065 12099 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
67547950 120851 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 456 6 0 3 4.9 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1C[N+]2(CCCn3cccc3)CCC1CC2 10.1016/j.bmcl.2015.02.065
CHEMBL3401655 120851 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 456 6 0 3 4.9 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1C[N+]2(CCCn3cccc3)CCC1CC2 10.1016/j.bmcl.2015.02.065
CHEMBL3559199 120851 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 456 6 0 3 4.9 CN(C(=O)C1c2ccccc2Oc2ccccc21)[C@H]1C[N+]2(CCCn3cccc3)CCC1CC2 10.1016/j.bmcl.2015.02.065
107782 14436 18 None -1 5 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
67151996 14436 18 None -1 5 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
CHEMBL1201207 14436 18 None -1 5 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
1224 1420 83 None -5 13 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1420 83 None -5 13 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1420 83 None -5 13 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1420 83 None -5 13 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1420 83 None -5 13 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1420 83 None -5 13 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3191 102831 97 None -6 25 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102831 97 None -6 25 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
54586723 62314 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 288 3 0 3 3.1 CC(C)N(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779038 62314 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 288 3 0 3 3.1 CC(C)N(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
1836 2574 59 None -42 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 2574 59 None -42 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 2574 59 None -42 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 2574 59 None -42 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 2574 59 None -42 15 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
10782321 12092 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.3 CCCCCc1noc(C2CN(CC)CC=C2c2ccccc2)n1 10.1021/jm980067l
CHEMBL1184098 12092 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.3 CCCCCc1noc(C2CN(CC)CC=C2c2ccccc2)n1 10.1021/jm980067l
CHEMBL332405 12092 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 325 7 0 4 4.3 CCCCCc1noc(C2CN(CC)CC=C2c2ccccc2)n1 10.1021/jm980067l
10854879 11385 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 4.9 CCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180239 11385 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 4.9 CCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL118241 11385 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 4.9 CCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
10636001 11393 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.1 CCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1180290 11393 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.1 CCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL120329 11393 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.1 CCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
10777692 11395 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.6 CCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180296 11395 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.6 CCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL120539 11395 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 259 4 0 3 2.6 CCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
3158 56237 27 None -104 20 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 56237 27 None -104 20 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
44233175 13987 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
CHEMBL1197209 13987 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
CHEMBL562655 13987 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 440 5 1 3 4.3 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C1(O)c2ccccc2-c2ccccc21 nan
50925543 19146 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4ccccc4Cl)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
CHEMBL1289654 19146 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 405 3 0 5 3.6 Cc1nc(C(=O)N2CCOC3(CCN(Cc4ccccc4Cl)CC3)C2)cs1 10.1016/j.bmcl.2010.10.016
57393502 69124 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 410 7 0 4 3.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCCC#N)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
CHEMBL1924045 69124 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrsDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs
ChEMBL 410 7 0 4 3.8 C[C@@](C(=O)O[C@H]1C[N+]2(CCCC#N)CCC1CC2)(c1ccccc1)N1CCCCC1 10.1016/j.bmcl.2011.10.002
76309856 103619 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 457 6 1 6 3.9 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1nncs1 10.1016/j.bmcl.2013.09.092
CHEMBL3087243 103619 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA methodDisplacement of [3H]NMS from recombinant human M3 receptor expressed in CHO-K1 cells after 16 hrs by SPA method
ChEMBL 457 6 1 6 3.9 O=C(C[N+]12CCC(CC1)[C@@H](OC(=O)C1(C3=CC=CC3)CCCCCC1)C2)Nc1nncs1 10.1016/j.bmcl.2013.09.092
10096508 176999 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 475 5 1 5 4.8 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCCC1 10.1021/jm00128a008
CHEMBL46315 176999 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligandBinding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand
ChEMBL 475 5 1 5 4.8 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCCC1 10.1021/jm00128a008
10096508 176999 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 475 5 1 5 4.8 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCCC1 10.1021/jm00048a014
CHEMBL46315 176999 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenatesInhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates
ChEMBL 475 5 1 5 4.8 CN(CC1CCCCN1CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C1CCCCCC1 10.1021/jm00048a014
54583839 62311 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 288 4 0 3 3.1 CCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779035 62311 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 288 4 0 3 3.1 CCCN(C(=O)O[C@H]1CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2011.03.096
118728611 117753 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 294 4 2 4 1.6 CCC(O)(C(=O)N[C@H]1CN2CCC1CC2)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401644 117753 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 294 4 2 4 1.6 CCC(O)(C(=O)N[C@H]1CN2CCC1CC2)c1cccs1 10.1016/j.bmcl.2015.02.065
9903030 62318 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 350 4 0 3 4.2 Cc1ccc(N(Cc2ccccc2)C(=O)O[C@H]2CN3CCC2CC3)cc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779042 62318 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 350 4 0 3 4.2 Cc1ccc(N(Cc2ccccc2)C(=O)O[C@H]2CN3CCC2CC3)cc1 10.1016/j.bmcl.2011.03.096
6726 1269 51 None -6 13 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 1269 51 None -6 13 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 1269 51 None -6 13 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 1269 51 None -6 13 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 1269 51 None -6 13 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
10784004 13355 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL1192621 13355 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
CHEMBL543890 13355 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 7 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccccc2)C1 10.1021/jm980067l
5282593 55228 26 None -1 5 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
CHEMBL1319362 55228 26 None -1 5 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
CHEMBL1618018 55228 26 None -1 5 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
44333822 4633 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 406 2 1 4 4.8 O=C1Nc2cccnc2N(C(=S)CC2CCCN3CCCC[C@@H]23)c2ccccc21 10.1016/s0960-894x(99)00528-4
CHEMBL103189 4633 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 406 2 1 4 4.8 O=C1Nc2cccnc2N(C(=S)CC2CCCN3CCCC[C@@H]23)c2ccccc21 10.1016/s0960-894x(99)00528-4
10048670 107431 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 436 4 1 5 4.3 O=C1Nc2cccnc2N(C(=O)CSCC2CCCN3CCCCC23)c2ccccc21 10.1016/s0960-894x(99)00528-4
CHEMBL318316 107431 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 436 4 1 5 4.3 O=C1Nc2cccnc2N(C(=O)CSCC2CCCN3CCCCC23)c2ccccc21 10.1016/s0960-894x(99)00528-4
1547484 937 74 None -5 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 937 74 None -5 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 937 74 None -5 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 937 74 None -5 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 937 74 None -5 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
135398737 955 93 None -10 92 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 955 93 None -10 92 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 955 93 None -10 92 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 955 93 None -10 92 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 955 93 None -10 92 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
52949883 19294 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 5 0 3 4.6 CCOc1ccccc1C(=O)N1CCC2(CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.10.016
CHEMBL1290634 19294 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 5 0 3 4.6 CCOc1ccccc1C(=O)N1CCC2(CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2010.10.016
54585742 62307 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 3 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
CHEMBL1779031 62307 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
ChEMBL 322 3 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.096
66592485 151202 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 500 9 2 7 4.4 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3O)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL3960065 151202 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 500 9 2 7 4.4 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3O)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
54673528 152732 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 790 15 6 11 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)[C@](O)(c3ccccc3)C3CCCC3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3973386 152732 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.Muscarinic Receptor Binding Assay: The study of binding to human muscarinic M1, M2, M3, M4 and M5 receptors was performed using commercial membranes (Perkin Elmer) prepared from CHO-K1 cells. Radioligand binding experiments were conducted in 96 polypropylene well plates in a total volume of 200 μl. All reagents were dissolved in assay binding buffer (PBS with calcium and magnesium, SIGMA), except compounds that were dissolved in DMSO 100%. Non-specific binding (NSB) was measured in the presence of 1 μM atropine. [3H]-NMS was used as the radioligand at a concentration of 1 nM for M2, M3 and M5 and 0.3 nM for M1 and M4. [3H]-NMS and antagonists were incubated with membranes that express human muscarinic receptors M1, M2, M3, M4 and M5 at concentrations of 8.1, 10, 4.9, 4.5 and 4.9 μg/well, respectively. After an incubation period of two hours with gentle shaking, 150 μl of the reaction mix were transferred to 96 GF/C filter plates (Millipore), previously treated with wash buffer (Tris 50 mM; NaCl 100 mM; pH: 7.4), containing 0.05% PEI (Sigma) during one hour. Bound and free [3H]-NMS were separated by rapid vacuum filtration in a manifold from Millipore and washed four times with ice cold wash buffer. After drying 30 min, 30 μl of OPTIPHASE Supermix were added to each well and radioactivity quantified using a Microbeta microplate scintillation counter.
ChEMBL 790 15 6 11 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)[C@](O)(c3ccccc3)C3CCCC3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
127053833 147775 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 7 0 4 5.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
CHEMBL3932738 147775 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 470 7 0 4 5.5 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C1c2ccccc2Oc2ccccc21 nan
44333541 4720 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 419 4 2 5 3.2 O=C1Nc2cccnc2N(C(=O)CNCC2CCCN3CCCCC23)c2ccccc21 10.1016/s0960-894x(99)00528-4
CHEMBL103785 4720 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.
ChEMBL 419 4 2 5 3.2 O=C1Nc2cccnc2N(C(=O)CNCC2CCCN3CCCCC23)c2ccccc21 10.1016/s0960-894x(99)00528-4
100826 90655 71 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity to M3 receptor (unknown origin) by radioligand displacement assayBinding affinity to M3 receptor (unknown origin) by radioligand displacement assay
ChEMBL 185 3 2 3 -0.6 CC(C)NC(=O)CN1CCNCC1 10.1016/j.bmc.2013.02.058
CHEMBL2391356 90655 71 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity to M3 receptor (unknown origin) by radioligand displacement assayBinding affinity to M3 receptor (unknown origin) by radioligand displacement assay
ChEMBL 185 3 2 3 -0.6 CC(C)NC(=O)CN1CCNCC1 10.1016/j.bmc.2013.02.058
2247 504 81 None -19 42 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 504 81 None -19 42 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 504 81 None -19 42 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 504 81 None -19 42 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 504 81 None -19 42 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
10827157 11405 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.2 CCN1CC=C(c2ccccc2)C(C(=O)OCC(C)C)C1 10.1021/jm980067l
CHEMBL1180317 11405 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.2 CCN1CC=C(c2ccccc2)C(C(=O)OCC(C)C)C1 10.1021/jm980067l
CHEMBL121552 11405 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 287 5 0 3 3.2 CCN1CC=C(c2ccccc2)C(C(=O)OCC(C)C)C1 10.1021/jm980067l
10854880 11389 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 5.1 CCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL1180282 11389 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 5.1 CCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
CHEMBL120080 11389 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 343 10 0 3 5.1 CCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1 10.1021/jm980067l
68835 72264 53 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity to M3 receptor (unknown origin) by radioligand displacement assayBinding affinity to M3 receptor (unknown origin) by radioligand displacement assay
ChEMBL 225 3 2 3 0.3 O=C(CN1CCNCC1)NC1CCCCC1 10.1016/j.bmc.2013.02.058
CHEMBL1983100 72264 53 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity to M3 receptor (unknown origin) by radioligand displacement assayBinding affinity to M3 receptor (unknown origin) by radioligand displacement assay
ChEMBL 225 3 2 3 0.3 O=C(CN1CCNCC1)NC1CCCCC1 10.1016/j.bmc.2013.02.058
10549581 11417 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.4 CCN1CC=C(c2ccccc2)C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
CHEMBL1180349 11417 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.4 CCN1CC=C(c2ccccc2)C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
CHEMBL123198 11417 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 411 7 0 3 5.4 CCN1CC=C(c2ccccc2)C(C(=O)OCC(c2ccccc2)c2ccccc2)C1 10.1021/jm980067l
10760249 11391 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm301774u
CHEMBL1180285 11391 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm301774u
CHEMBL120119 11391 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M3 muscarinic receptor expressed in cell membranes by radioligand binding assay
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm301774u
10760249 11391 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
CHEMBL1180285 11391 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
CHEMBL120119 11391 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1 10.1021/jm980067l
2551 791 23 None -346 11 Human 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
298 791 23 None -346 11 Human 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
488 791 23 None -346 11 Human 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
CHEMBL965 791 23 None -346 11 Human 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
DB00411 791 23 None -346 11 Human 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS radioligand using membranes from transfected chinese hamster ovarian cell
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00351-5
10538337 12079 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.2 CCN1CC=C(c2ccccc2)C(C(=O)OC)C1 10.1021/jm980067l
CHEMBL1184062 12079 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.2 CCN1CC=C(c2ccccc2)C(C(=O)OC)C1 10.1021/jm980067l
CHEMBL330885 12079 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 245 3 0 3 2.2 CCN1CC=C(c2ccccc2)C(C(=O)OC)C1 10.1021/jm980067l
118728611 117753 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 294 4 2 4 1.6 CCC(O)(C(=O)N[C@H]1CN2CCC1CC2)c1cccs1 10.1016/j.bmcl.2015.02.065
CHEMBL3401644 117753 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting methodDisplacement of [3H]NMS from human M3 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
ChEMBL 294 4 2 4 1.6 CCC(O)(C(=O)N[C@H]1CN2CCC1CC2)c1cccs1 10.1016/j.bmcl.2015.02.065
66592447 147678 0 None - 0 Human 8.0 pIC50 = 8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.4 O=C(O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
CHEMBL3931995 147678 0 None - 0 Human 8.0 pIC50 = 8 Binding
[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.[3H]-NMS Binding Assay: The binding of [3H]-NMS to human muscarinic receptors was performed according to Waelbroek et al (1990) (1). Assays were carried out at 25° C. Membrane preparations from stably transfected chinese hamster ovary-K1 cells (CHO) expressing the genes for the human muscarinic receptors Hm3 were used.
ChEMBL 484 9 1 6 4.4 O=C(O[C@H]1C[N+]2(CCOCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 nan
100 3776 58 None -8 56 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3776 58 None -8 56 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3776 58 None -8 56 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3776 58 None -8 56 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3776 58 None -8 56 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2551 791 23 None -346 11 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
298 791 23 None -346 11 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
488 791 23 None -346 11 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
CHEMBL965 791 23 None -346 11 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
DB00411 791 23 None -346 11 Human 5.0 pIC50 = 5.0 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9702903
10638050 11383 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.8 CCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL116601 11383 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.8 CCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180202 11383 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 301 7 0 3 3.8 CCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
44235638 195291 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 347 2 0 3 3.6 O=C(O[C@H]1CN2CCC1CC2)C1c2ccccc2CCc2ccccc21 10.1021/jm900132z
CHEMBL551525 195291 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHOK1 cells by microplate scintillation counting
ChEMBL 347 2 0 3 3.6 O=C(O[C@H]1CN2CCC1CC2)C1c2ccccc2CCc2ccccc21 10.1021/jm900132z
11498 2997 41 None -38 6 Human 6.0 pIC50 = 6.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/s0960-894x(98)00351-5
4995951 2997 41 None -38 6 Human 6.0 pIC50 = 6.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/s0960-894x(98)00351-5
CHEMBL59898 2997 41 None -38 6 Human 6.0 pIC50 = 6.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/s0960-894x(98)00351-5
2200 3109 46 None -7 13 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
328 3109 46 None -7 13 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
4848 3109 46 None -7 13 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
CHEMBL9967 3109 46 None -7 13 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
DB00670 3109 46 None -7 13 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm980067l
10846833 49775 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 225 0 0 5 1.7 CN1CCC2=C(C1)c1nsnc1SC2 10.1021/jm9705216
CHEMBL15675 49775 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
ChEMBL 225 0 0 5 1.7 CN1CCC2=C(C1)c1nsnc1SC2 10.1021/jm9705216
10547222 114760 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.7 CCCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333940 114760 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cellsDisplacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.7 CCCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
2812 4747 101 None -22 34 Human 5.0 pIC50 = 5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4747 101 None -22 34 Human 5.0 pIC50 = 5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
164612037 185353 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 185353 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
168290235 192944 0 None -8 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192944 0 None -8 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192944 0 None -8 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294767 192995 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192995 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192995 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168295528 193007 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 193007 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 193007 0 None -2 20 Human 9.9 pKd = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic acetylcholine M3 receptor stably expressed in CHO cells by radioligand competition binding based analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
4120 5902 6 None 1 3 Rat 9.4 pKd = 9.4 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 318 4 1 4 1.1 C[N+]1(C)C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL107979 5902 6 None 1 3 Rat 9.4 pKd = 9.4 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 318 4 1 4 1.1 C[N+]1(C)C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL293927 5902 6 None 1 3 Rat 9.4 pKd = 9.4 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 318 4 1 4 1.1 C[N+]1(C)C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
174174 521 49 None -1 14 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00170a010
260 521 49 None -1 14 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00170a010
320 521 49 None -1 14 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00170a010
CHEMBL517712 521 49 None -1 14 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00170a010
DB00572 521 49 None -1 14 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00170a010
11968014 12726 5 None -1 9 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/jm00170a010
CHEMBL1187846 12726 5 None -1 9 Rat 9.2 pKd = 9.2 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/jm00170a010
14753629 13636 0 None -1 3 Rat 8.9 pKd = 8.9 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 302 5 2 4 1.9 N=CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL1194660 13636 0 None -1 3 Rat 8.9 pKd = 8.9 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 302 5 2 4 1.9 N=CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL553066 13636 0 None -1 3 Rat 8.9 pKd = 8.9 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 302 5 2 4 1.9 N=CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
9913341 82129 4 None -25 5 Human 6.8 pKd = 6.8 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL216927 82129 4 None -25 5 Human 6.8 pKd = 6.8 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL553058 82129 4 None -25 5 Human 6.8 pKd = 6.8 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
44418764 82130 0 None -8 5 Human 6.8 pKd = 6.8 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
CHEMBL216928 82130 0 None -8 5 Human 6.8 pKd = 6.8 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
14753624 13704 0 None 2 3 Rat 8.6 pKd = 8.6 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 317 4 3 4 1.2 N=C(N)N1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL1195123 13704 0 None 2 3 Rat 8.6 pKd = 8.6 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 317 4 3 4 1.2 N=C(N)N1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL553894 13704 0 None 2 3 Rat 8.6 pKd = 8.6 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 317 4 3 4 1.2 N=C(N)N1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
5861 11253 11 None -1 3 Rat 8.6 pKd = 8.6 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 304 4 1 3 2.1 C[N+]1(C)C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL1179176 11253 11 None -1 3 Rat 8.6 pKd = 8.6 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 304 4 1 3 2.1 C[N+]1(C)C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL63452 11253 11 None -1 3 Rat 8.6 pKd = 8.6 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 304 4 1 3 2.1 C[N+]1(C)C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
3636 11115 5 None -1 3 Rat 6.7 pKd = 6.7 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 360 7 1 4 2.2 CCCC[N+]1(C)C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL1178342 11115 5 None -1 3 Rat 6.7 pKd = 6.7 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 360 7 1 4 2.2 CCCC[N+]1(C)C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL21823 11115 5 None -1 3 Rat 6.7 pKd = 6.7 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 360 7 1 4 2.2 CCCC[N+]1(C)C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL5285607 194281 0 None -1 5 Human 7.6 pKd = 7.6 Binding
Binding affinity to saturated human muscarinic M3 expressed in CHO cells assessed as dissociation constant incubated for 2 hrs by flow cytometryBinding affinity to saturated human muscarinic M3 expressed in CHO cells assessed as dissociation constant incubated for 2 hrs by flow cytometry
ChEMBL 1052 21 1 13 10.0 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
CHEMBL5285607 194281 0 None -1 5 Human 7.6 pKd = 7.6 Binding
Binding affinity to saturated human muscarinic M3 expressed in CHO cells assessed as dissociation constant incubated for 2 hrs in presence of atropine by flow cytometryBinding affinity to saturated human muscarinic M3 expressed in CHO cells assessed as dissociation constant incubated for 2 hrs in presence of atropine by flow cytometry
ChEMBL 1052 21 1 13 10.0 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
14753634 13695 0 None -1 3 Rat 8.5 pKd = 8.5 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 316 4 2 4 2.3 CC(=N)N1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL1195059 13695 0 None -1 3 Rat 8.5 pKd = 8.5 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 316 4 2 4 2.3 CC(=N)N1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
CHEMBL553783 13695 0 None -1 3 Rat 8.5 pKd = 8.5 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 316 4 2 4 2.3 CC(=N)N1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 10.1021/jm00170a010
14753637 13457 0 None -1 3 Rat 8.5 pKd = 8.5 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 330 4 2 5 1.3 CC(=N)N1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL1193366 13457 0 None -1 3 Rat 8.5 pKd = 8.5 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 330 4 2 5 1.3 CC(=N)N1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL544759 13457 0 None -1 3 Rat 8.5 pKd = 8.5 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 330 4 2 5 1.3 CC(=N)N1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
14753627 13674 0 None 1 3 Rat 8.4 pKd = 8.4 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 331 4 3 5 0.2 N=C(N)N1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL1194941 13674 0 None 1 3 Rat 8.4 pKd = 8.4 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 331 4 3 5 0.2 N=C(N)N1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL553562 13674 0 None 1 3 Rat 8.4 pKd = 8.4 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 331 4 3 5 0.2 N=C(N)N1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL5271406 193657 0 None -3 5 Human 7.3 pKd = 7.3 Binding
Binding affinity to saturated human muscarinic M3 expressed in CHO cells assessed as dissociation constant incubated for 2 hrs in presence of atropine by flow cytometryBinding affinity to saturated human muscarinic M3 expressed in CHO cells assessed as dissociation constant incubated for 2 hrs in presence of atropine by flow cytometry
ChEMBL 1159 27 3 10 12.8 CC1(C)C(/C=C/C=C/C=C2/N(CCCCS(=O)(=O)O)c3ccccc3C2(C)C)=[N+](CCCCCC(=O)NCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(F)c(Cl)c3)CC2)c2ccc(S(=O)(=O)[O-])cc21 10.1021/acs.jmedchem.2c01376
14753632 13476 0 None -1 3 Rat 8.3 pKd = 8.3 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 316 5 2 5 0.9 N=CN1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL1193564 13476 0 None -1 3 Rat 8.3 pKd = 8.3 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 316 5 2 5 0.9 N=CN1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL544993 13476 0 None -1 3 Rat 8.3 pKd = 8.3 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
ChEMBL 316 5 2 5 0.9 N=CN1C2CC(OC(=O)C(CO)c3ccccc3)CC1C1OC12 10.1021/jm00170a010
CHEMBL5271406 193657 0 None -3 5 Human 7.3 pKd = 7.3 Binding
Binding affinity to saturated human muscarinic M3 expressed in CHO cells assessed as dissociation constant incubated for 2 hrs by flow cytometryBinding affinity to saturated human muscarinic M3 expressed in CHO cells assessed as dissociation constant incubated for 2 hrs by flow cytometry
ChEMBL 1159 27 3 10 12.8 CC1(C)C(/C=C/C=C/C=C2/N(CCCCS(=O)(=O)O)c3ccccc3C2(C)C)=[N+](CCCCCC(=O)NCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(F)c(Cl)c3)CC2)c2ccc(S(=O)(=O)[O-])cc21 10.1021/acs.jmedchem.2c01376
16094788 141890 0 None -125 5 Human 7.2 pKd = 7.2 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL386983 141890 0 None -125 5 Human 7.2 pKd = 7.2 Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol bindingAntagonist activity at human M3 receptor assessed as inhibition of carbachol binding
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
367 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Antagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assayAntagonist activity at human M3 receptor expressed in CHO cells assessed as inhibition of carbachol-induced response after 30 mins by AP-1-driven luciferase reporter gene assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 D518A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K213A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 K523A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3795 12 None 2 8 Human 11.0 pKi = 11 Binding
Binding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 R133A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
9874175 58508 1 None 34 2 Human 11.0 pKi = 11 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683934 58508 1 None 34 2 Human 11.0 pKi = 11 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
367 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E220A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F222A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 F225A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3795 12 None 2 8 Human 10.8 pKi = 10.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
367 3795 12 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3795 12 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3795 12 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3795 12 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3795 12 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3795 12 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3795 12 None 2 8 Human 10.7 pKi = 10.7 Binding
Binding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 E228A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
59291417 112796 0 None -1 3 Rat 10.7 pKi = 10.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 343 3 1 3 4.3 C[N+]12CCC(OC(=O)Nc3ccsc3-c3ccccc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298595 112796 0 None -1 3 Rat 10.7 pKi = 10.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 343 3 1 3 4.3 C[N+]12CCC(OC(=O)Nc3ccsc3-c3ccccc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3307168 112796 0 None -1 3 Rat 10.7 pKi = 10.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 343 3 1 3 4.3 C[N+]12CCC(OC(=O)Nc3ccsc3-c3ccccc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
367 3795 12 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
5487427 3795 12 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
8592 3795 12 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL1900528 3795 12 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3305968 3795 12 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL4650755 3795 12 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB01409 3795 12 None 2 8 Human 10.6 pKi = 10.6 Binding
Binding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to human M3 Q224A mutant expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
11504490 192578 0 None 39 3 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
CHEMBL521523 192578 0 None 39 3 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 514 8 3 4 4.8 C[C@H]1CN(Cc2cccc(-c3cc(CNC(=O)c4cccc(CC5CCNCC5)c4)ccc3F)c2)CCN1 10.1021/jm800935u
367 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
5487427 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
8592 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
CHEMBL1900528 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
CHEMBL3305968 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
CHEMBL4650755 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
DB01409 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm501915g
367 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
5487427 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
8592 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
CHEMBL1900528 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
CHEMBL3305968 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
CHEMBL4650755 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
DB01409 3795 12 None 2 8 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2011.01.043
25005841 112793 0 None -1 3 Rat 10.3 pKi = 10.3 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 378 3 1 4 4.4 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cccc(Cl)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298599 112793 0 None -1 3 Rat 10.3 pKi = 10.3 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 378 3 1 4 4.4 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cccc(Cl)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3307130 112793 0 None -1 3 Rat 10.3 pKi = 10.3 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 378 3 1 4 4.4 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cccc(Cl)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
10109130 132990 0 None 6 2 Human 10.3 pKi = 10.3 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 359 3 1 5 3.2 CO[C@]1(C#CC(O)(c2cccs2)c2cccs2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL370232 132990 0 None 6 2 Human 10.3 pKi = 10.3 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 359 3 1 5 3.2 CO[C@]1(C#CC(O)(c2cccs2)c2cccs2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
72712272 106428 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 390 4 0 5 3.4 CC(C(=O)O[C@@H]1C[C@H]2[C@@H]3O[C@@H]3[C@@H](C1)[N+]2(C)C)(c1cccs1)c1cccs1 10.1021/jm401219y
CHEMBL3091665 106428 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 390 4 0 5 3.4 CC(C(=O)O[C@@H]1C[C@H]2[C@@H]3O[C@@H]3[C@@H](C1)[N+]2(C)C)(c1cccs1)c1cccs1 10.1021/jm401219y
CHEMBL3139995 106428 0 None - 1 Human 10.3 pKi = 10.3 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 390 4 0 5 3.4 CC(C(=O)O[C@@H]1C[C@H]2[C@@H]3O[C@@H]3[C@@H](C1)[N+]2(C)C)(c1cccs1)c1cccs1 10.1021/jm401219y
11857427 119026 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426693 119026 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
59291402 112759 0 None 1 3 Rat 10.3 pKi = 10.3 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1ccsc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298588 112759 0 None 1 3 Rat 10.3 pKi = 10.3 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1ccsc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305766 112759 0 None 1 3 Rat 10.3 pKi = 10.3 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1ccsc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
25195533 78357 2 None -1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2103803 78357 2 None -1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2110584 78357 2 None -1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
11519069 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
11519070 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
4816 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
7354 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
CHEMBL1187833 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
DB09076 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm801601v
72712270 106427 0 None - 1 Human 10.2 pKi = 10.2 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 380 4 1 4 2.2 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)(c3ccccc3)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3091664 106427 0 None - 1 Human 10.2 pKi = 10.2 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 380 4 1 4 2.2 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)(c3ccccc3)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3139994 106427 0 None - 1 Human 10.2 pKi = 10.2 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 380 4 1 4 2.2 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)(c3ccccc3)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL5074599 214296 2 None 2 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
12165 908 6 None -15 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 10.1021/acs.jmedchem.2c00609
90200922 908 6 None -15 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 10.1021/acs.jmedchem.2c00609
CHEMBL5172865 908 6 None -15 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 10.1021/acs.jmedchem.2c00609
90213810 191239 0 None -2 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 750 16 5 11 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)o2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5190387 191239 0 None -2 2 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 750 16 5 11 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)o2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
25195533 78357 2 None -1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2103803 78357 2 None -1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2110584 78357 2 None -1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 345 4 0 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
59291241 112788 0 None -1 3 Rat 10.2 pKi = 10.2 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 344 3 1 4 3.7 C[N+]12CCC(OC(=O)Nc3ncsc3-c3ccccc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298596 112788 0 None -1 3 Rat 10.2 pKi = 10.2 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 344 3 1 4 3.7 C[N+]12CCC(OC(=O)Nc3ncsc3-c3ccccc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3307116 112788 0 None -1 3 Rat 10.2 pKi = 10.2 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 344 3 1 4 3.7 C[N+]12CCC(OC(=O)Nc3ncsc3-c3ccccc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
156011965 177268 0 None 3 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.2c01376
CHEMBL4636528 177268 0 None 3 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.2c01376
156011965 177268 0 None 3 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636528 177268 0 None 3 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
11434515 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
11519741 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
4484 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
7449 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
CHEMBL1194325 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
DB08897 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1021/jm900132z
10143956 13879 0 None -1 3 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL1196359 13879 0 None -1 3 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
CHEMBL556635 13879 0 None -1 3 Human 10.2 pKi = 10.2 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 470 9 1 5 4.7 O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)[C@](O)(c1cccs1)C1CCCC1 10.1021/jm900132z
156009673 178230 0 None 1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4633816 178230 0 None 1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650683 178230 0 None 1 3 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
156014812 178238 0 None 1 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4647437 178238 0 None 1 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650736 178238 0 None 1 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
367 3795 12 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
5487427 3795 12 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
8592 3795 12 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL1900528 3795 12 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL3305968 3795 12 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
CHEMBL4650755 3795 12 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
DB01409 3795 12 None 2 8 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm200884j
168287036 191482 0 None -3 2 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5193853 191482 0 None -3 2 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
10372344 119020 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 675 12 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
CHEMBL3426687 119020 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 675 12 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
10291977 72869 0 None 5 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 359 3 1 5 3.2 CO[C@]1(C#CC(O)(c2ccsc2)c2ccsc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200401 72869 0 None 5 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 359 3 1 5 3.2 CO[C@]1(C#CC(O)(c2ccsc2)c2ccsc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
11852298 13994 0 None -1 3 Human 10.1 pKi = 10.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL1197251 13994 0 None -1 3 Human 10.1 pKi = 10.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL564057 13994 0 None -1 3 Human 10.1 pKi = 10.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 454 7 1 5 4.4 O=C(O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1 10.1021/jm900132z
CHEMBL5281043 194076 0 None 5 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 479 10 2 4 6.1 NCCCCCCN1CCC(COC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c01376
156015300 177568 0 None 4 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640703 177568 0 None 4 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
54580128 61764 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 723 20 6 7 7.2 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(CO)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773196 61764 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 723 20 6 7 7.2 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(CO)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
15599352 108596 0 None -2 2 Rat 10.0 pKi = 10.0 Binding
The compound was tested for binding activity against muscarinic acetylcholine receptor M3, using [3H]-QNB as the radioligand.The compound was tested for binding activity against muscarinic acetylcholine receptor M3, using [3H]-QNB as the radioligand.
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL320611 108596 0 None -2 2 Rat 10.0 pKi = 10.0 Binding
The compound was tested for binding activity against muscarinic acetylcholine receptor M3, using [3H]-QNB as the radioligand.The compound was tested for binding activity against muscarinic acetylcholine receptor M3, using [3H]-QNB as the radioligand.
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL5070876 214223 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5076637 214431 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3F)s2)cc1OC 10.1021/acs.jmedchem.1c00204
164620727 186062 0 None -7 2 Human 10.0 pKi = 10 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 821 16 6 9 6.8 O=C(N[C@@H](c1ccccc1)c1ccc(-c2cccc(OCc3ccc(C(=O)NCCCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)c2)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4871517 186062 0 None -7 2 Human 10.0 pKi = 10 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 821 16 6 9 6.8 O=C(N[C@@H](c1ccccc1)c1ccc(-c2cccc(OCc3ccc(C(=O)NCCCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)c2)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
59291493 112795 0 None -1 3 Rat 10.0 pKi = 10 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 362 3 1 4 3.9 C[N+]12CCC(OC(=O)Nc3ncsc3-c3ccc(F)cc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298600 112795 0 None -1 3 Rat 10.0 pKi = 10 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 362 3 1 4 3.9 C[N+]12CCC(OC(=O)Nc3ncsc3-c3ccc(F)cc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3307158 112795 0 None -1 3 Rat 10.0 pKi = 10 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 362 3 1 4 3.9 C[N+]12CCC(OC(=O)Nc3ncsc3-c3ccc(F)cc3)(CC1)CC2 10.1016/j.bmc.2014.04.031
10461973 119030 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 655 15 6 8 4.9 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)NCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426697 119030 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 655 15 6 8 4.9 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)NCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
87142783 119037 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3426704 119037 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548101 124373 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3639442 124373 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548063 125175 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645274 125175 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548134 125176 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645275 125176 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057795 125177 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645276 125177 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
66791483 125178 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645277 125178 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548074 125179 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645278 125179 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548089 125180 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645279 125180 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548094 125181 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645280 125181 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548099 125182 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645281 125182 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
68057677 125183 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645282 125183 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548122 125184 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 17 6 9 6.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645283 125184 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 17 6 9 6.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548079 125185 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645284 125185 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548056 125186 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645285 125186 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548067 125187 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645286 125187 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548141 125188 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645287 125188 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548102 125189 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645288 125189 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057804 125190 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645289 125190 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548054 125191 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645290 125191 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548125 125192 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645291 125192 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548107 125194 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645293 125194 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548081 125196 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645295 125196 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548093 125199 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645298 125199 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548138 125207 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645305 125207 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548130 125210 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645308 125210 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548100 125211 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645309 125211 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
66791606 125213 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645311 125213 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843742 125216 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645314 125216 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548073 125227 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645324 125227 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548112 125228 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645325 125228 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548061 125229 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645326 125229 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548066 125230 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645327 125230 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548076 125231 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645328 125231 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548117 125233 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645330 125233 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548121 125235 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645332 125235 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548110 125236 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645333 125236 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548135 125238 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645335 125238 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548142 125245 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645341 125245 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548083 125247 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645343 125247 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548140 125249 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645345 125249 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548050 125250 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645346 125250 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548069 125252 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645348 125252 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548115 125254 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645350 125254 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548103 125255 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645351 125255 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548057 125256 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645352 125256 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548090 125260 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
CHEMBL3645356 125260 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
59548133 125262 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645358 125262 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548068 125263 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645359 125263 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548105 125265 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645361 125265 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548071 125266 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645362 125266 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
56953428 125267 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645363 125267 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
49785227 125269 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645365 125269 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
49785225 128441 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 17 6 9 7.0 Cc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3666068 128441 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 17 6 9 7.0 Cc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
49785142 143247 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 18 6 9 5.8 C[C@@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3896828 143247 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 816 18 6 9 5.8 C[C@@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
118405970 151781 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 848 17 5 8 7.6 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NCCc1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3965175 151781 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 848 17 5 8 7.6 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NCCc1ccc(O)c2[nH]c(=O)ccc12 nan
118405964 160755 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.3 C[C@@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)c1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1 nan
CHEMBL4114219 160755 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.3 C[C@@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)c1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1 nan
59548101 124373 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3639442 124373 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548063 125175 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645274 125175 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548134 125176 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645275 125176 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057795 125177 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645276 125177 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
66791483 125178 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645277 125178 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548074 125179 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645278 125179 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548089 125180 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645279 125180 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548094 125181 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645280 125181 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548099 125182 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645281 125182 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
68057677 125183 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645282 125183 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548122 125184 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 17 6 9 6.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645283 125184 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 17 6 9 6.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548079 125185 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645284 125185 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548056 125186 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645285 125186 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548067 125187 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645286 125187 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548141 125188 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645287 125188 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548102 125189 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645288 125189 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057804 125190 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645289 125190 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548054 125191 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645290 125191 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548125 125192 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645291 125192 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548107 125194 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645293 125194 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548081 125196 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645295 125196 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548093 125199 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645298 125199 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548138 125207 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645305 125207 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548130 125210 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645308 125210 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548100 125211 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645309 125211 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
66791606 125213 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645311 125213 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843742 125216 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645314 125216 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843735 125220 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.4 CC(Cc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645318 125220 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.4 CC(Cc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548065 125225 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645322 125225 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548073 125227 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645324 125227 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548112 125228 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645325 125228 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548061 125229 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645326 125229 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548066 125230 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645327 125230 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548076 125231 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645328 125231 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548117 125233 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645330 125233 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548058 125234 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645331 125234 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548121 125235 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645332 125235 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548110 125236 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645333 125236 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548135 125238 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645335 125238 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548142 125245 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645341 125245 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548083 125247 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645343 125247 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548140 125249 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645345 125249 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548050 125250 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645346 125250 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548069 125252 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645348 125252 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548103 125255 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645351 125255 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548057 125256 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645352 125256 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548090 125260 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
CHEMBL3645356 125260 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
59548133 125262 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645358 125262 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548068 125263 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645359 125263 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
91667374 125264 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 17 6 9 6.4 C[C@@H](Cc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645360 125264 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 802 17 6 9 6.4 C[C@@H](Cc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548105 125265 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645361 125265 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548071 125266 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645362 125266 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
56953428 125267 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645363 125267 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548055 125268 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 808 14 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645364 125268 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 808 14 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
49785227 125269 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645365 125269 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548101 124373 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3639442 124373 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548063 125175 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645274 125175 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548134 125176 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645275 125176 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057795 125177 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645276 125177 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
66791483 125178 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645277 125178 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548074 125179 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645278 125179 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548089 125180 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645279 125180 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548094 125181 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645280 125181 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548099 125182 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645281 125182 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
68057677 125183 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645282 125183 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548079 125185 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645284 125185 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548056 125186 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645285 125186 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548067 125187 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645286 125187 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548141 125188 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645287 125188 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548102 125189 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645288 125189 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057804 125190 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645289 125190 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548054 125191 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645290 125191 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548125 125192 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645291 125192 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548107 125194 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645293 125194 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548081 125196 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645295 125196 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548093 125199 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645298 125199 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
49785226 125202 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645300 125202 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548138 125207 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645305 125207 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548130 125210 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645308 125210 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548100 125211 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645309 125211 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
66791606 125213 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645311 125213 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843742 125216 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645314 125216 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843735 125220 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.4 CC(Cc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645318 125220 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.4 CC(Cc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548065 125225 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645322 125225 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548073 125227 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645324 125227 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548112 125228 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645325 125228 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548061 125229 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645326 125229 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548066 125230 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645327 125230 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548076 125231 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645328 125231 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548117 125233 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645330 125233 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548058 125234 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645331 125234 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548121 125235 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645332 125235 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548110 125236 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645333 125236 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548135 125238 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645335 125238 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548142 125245 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645341 125245 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548083 125247 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645343 125247 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548140 125249 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645345 125249 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548050 125250 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645346 125250 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548069 125252 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645348 125252 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548103 125255 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645351 125255 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548057 125256 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645352 125256 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548090 125260 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
CHEMBL3645356 125260 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
59548133 125262 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645358 125262 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548068 125263 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645359 125263 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548071 125266 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645362 125266 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
56953428 125267 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645363 125267 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548055 125268 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 808 14 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645364 125268 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 808 14 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
49785227 125269 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645365 125269 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
90654070 128439 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1cccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3666066 128439 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1cccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
90654071 128440 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 17 6 9 5.9 C[C@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)c1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3666067 128440 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 802 17 6 9 5.9 C[C@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)c1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
49785225 128441 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 816 17 6 9 7.0 Cc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3666068 128441 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 816 17 6 9 7.0 Cc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
16065402 67898 0 None -1 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 428 9 1 3 4.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910848 67898 0 None -1 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 428 9 1 3 4.8 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2ccccc2)C1 10.1021/jm200884j
174174 521 49 None -1 14 Rat 9.9 pKi = 9.9 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00059a009
260 521 49 None -1 14 Rat 9.9 pKi = 9.9 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00059a009
320 521 49 None -1 14 Rat 9.9 pKi = 9.9 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00059a009
CHEMBL517712 521 49 None -1 14 Rat 9.9 pKi = 9.9 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00059a009
DB00572 521 49 None -1 14 Rat 9.9 pKi = 9.9 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm00059a009
59291527 112436 1 None 2 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1sccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298333 112436 1 None 2 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1sccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
25006208 112798 0 None -1 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 412 3 1 4 5.0 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cc(Cl)cc(Cl)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298763 112798 0 None -1 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 412 3 1 4 5.0 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cc(Cl)cc(Cl)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3307197 112798 0 None -1 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 412 3 1 4 5.0 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cc(Cl)cc(Cl)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
367 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
5487427 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
8592 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
CHEMBL1900528 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
CHEMBL3305968 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
CHEMBL4650755 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
DB01409 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.1c00204
CHEMBL5074216 214292 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@@H]3CCN(C)C3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5074599 214296 2 None 2 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5091461 215286 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3F)s2)cc1OC 10.1021/acs.jmedchem.1c00204
164613832 184515 0 None 3 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 654 15 5 8 5.4 O=C(N[C@@H](c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4847910 184515 0 None 3 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 654 15 5 8 5.4 O=C(N[C@@H](c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164615119 184949 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 688 13 5 8 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4854091 184949 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 688 13 5 8 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164622948 186080 0 None -1 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 911 18 5 9 8.7 O=C(N[C@@H](c1ccccc1)c1ccc(-c2cccc(OCc3ccc(C(=O)N(CCCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)Cc4ccccc4)cc3)c2)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4871702 186080 0 None -1 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 911 18 5 9 8.7 O=C(N[C@@H](c1ccccc1)c1ccc(-c2cccc(OCc3ccc(C(=O)N(CCCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)Cc4ccccc4)cc3)c2)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164615119 184949 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 688 13 5 8 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL4854091 184949 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 688 13 5 8 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
168280960 190824 0 None -6 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5184455 190824 0 None -6 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
10291366 140674 0 None 4 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 1 3 3.0 CO[C@]1(C#CC(O)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL381623 140674 0 None 4 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 1 3 3.0 CO[C@]1(C#CC(O)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
9874175 58508 1 None 34 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
CHEMBL1683934 58508 1 None 34 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
16065403 67906 23 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910856 67906 23 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1 10.1021/jm200884j
71452756 79512 0 None -4 4 Human 9.9 pKi = 9.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 423 6 0 3 5.9 C=C(c1ccc([S@@+]([O-])c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
CHEMBL2114068 79512 0 None -4 4 Human 9.9 pKi = 9.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 423 6 0 3 5.9 C=C(c1ccc([S@@+]([O-])c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
10291366 140674 0 None 4 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 347 3 1 3 3.0 CO[C@]1(C#CC(O)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL381623 140674 0 None 4 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 347 3 1 3 3.0 CO[C@]1(C#CC(O)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
11691950 12730 0 None 2 3 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187853 12730 0 None 2 3 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL524097 12730 0 None 2 3 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assayDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity assay
ChEMBL 428 8 1 2 5.4 OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCCOc3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL5285607 194281 0 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of tiotropium bromide from human muscarinic M3 receptor expressed in CHO cells incubated for 4 hrs by flow cytometric competition binding assayDisplacement of tiotropium bromide from human muscarinic M3 receptor expressed in CHO cells incubated for 4 hrs by flow cytometric competition binding assay
ChEMBL 1052 21 1 13 10.0 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
316 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm061374r
317 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm061374r
71183 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm061374r
CHEMBL3140030 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm061374r
CHEMBL376897 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm061374r
DB00462 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm061374r
316 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm2013216
317 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm2013216
71183 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm2013216
CHEMBL3140030 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm2013216
CHEMBL376897 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm2013216
DB00462 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm2013216
316 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm901048j
317 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm901048j
71183 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm901048j
CHEMBL3140030 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm901048j
CHEMBL376897 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm901048j
DB00462 2816 19 None -2 9 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm901048j
367 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
5487427 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
8592 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL1900528 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL3305968 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
CHEMBL4650755 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
DB01409 3795 12 None 2 8 Human 9.9 pKi = 9.9 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm900132z
10348864 58509 0 None 147 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 616 18 5 7 6.7 O=CNc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1016/j.bmcl.2011.01.043
CHEMBL1683935 58509 0 None 147 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 616 18 5 7 6.7 O=CNc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1016/j.bmcl.2011.01.043
10054373 58510 0 None 436 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 603 17 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683936 58510 0 None 436 2 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 603 17 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)CC1 10.1016/j.bmcl.2011.01.043
9798900 63106 1 None 2 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 322 3 1 3 4.1 O=C(Nc1ccccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL1779047 63106 1 None 2 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 322 3 1 3 4.1 O=C(Nc1ccccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL1789446 63106 1 None 2 3 Rat 9.9 pKi = 9.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 322 3 1 3 4.1 O=C(Nc1ccccc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL5271406 193657 0 None -3 5 Human 9.9 pKi = 9.9 Binding
Displacement of tiotropium bromide from human muscarinic M3 receptor expressed in CHO cells incubated for 4 hrs by flow cytometric competition binding assayDisplacement of tiotropium bromide from human muscarinic M3 receptor expressed in CHO cells incubated for 4 hrs by flow cytometric competition binding assay
ChEMBL 1159 27 3 10 12.8 CC1(C)C(/C=C/C=C/C=C2/N(CCCCS(=O)(=O)O)c3ccccc3C2(C)C)=[N+](CCCCCC(=O)NCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(F)c(Cl)c3)CC2)c2ccc(S(=O)(=O)[O-])cc21 10.1021/acs.jmedchem.2c01376
CHEMBL5271406 193657 0 None -3 5 Human 9.8 pKi = 9.8 Binding
Displacement of tiotropium bromide from human muscarinic M3 receptor expressed in CHO cells incubated for 4 hrs by flow cytometric competition binding assayDisplacement of tiotropium bromide from human muscarinic M3 receptor expressed in CHO cells incubated for 4 hrs by flow cytometric competition binding assay
ChEMBL 1159 27 3 10 12.8 CC1(C)C(/C=C/C=C/C=C2/N(CCCCS(=O)(=O)O)c3ccccc3C2(C)C)=[N+](CCCCCC(=O)NCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(F)c(Cl)c3)CC2)c2ccc(S(=O)(=O)[O-])cc21 10.1021/acs.jmedchem.2c01376
CHEMBL5270870 193633 0 None 2 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 507 12 2 4 6.8 NCCCCCCCCN1CCC(COC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c01376
CHEMBL5285607 194281 0 None -1 5 Human 9.8 pKi = 9.8 Binding
Displacement of tiotropium bromide from human muscarinic M3 receptor expressed in CHO cells incubated for 4 hrs by flow cytometric competition binding assayDisplacement of tiotropium bromide from human muscarinic M3 receptor expressed in CHO cells incubated for 4 hrs by flow cytometric competition binding assay
ChEMBL 1052 21 1 13 10.0 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
316 2816 19 None -2 9 Human 9.8 pKi = 9.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
317 2816 19 None -2 9 Human 9.8 pKi = 9.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
71183 2816 19 None -2 9 Human 9.8 pKi = 9.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL3140030 2816 19 None -2 9 Human 9.8 pKi = 9.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL376897 2816 19 None -2 9 Human 9.8 pKi = 9.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
DB00462 2816 19 None -2 9 Human 9.8 pKi = 9.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/jm401219y
CHEMBL5075132 214336 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)cc2F)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5076558 214425 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2cccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5076637 214431 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3F)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5077161 214463 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)cc2)cc1OC 10.1021/acs.jmedchem.1c00204
164617389 184847 0 None 1 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 682 17 5 8 6.2 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4852629 184847 0 None 1 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 682 17 5 8 6.2 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
168296356 192461 0 None -3 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 751 16 5 12 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5208957 192461 0 None -3 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 751 16 5 12 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
44232952 103356 0 None -3 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084650 103356 0 None -3 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 330 4 0 2 4.8 CN1[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
118737348 119024 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426691 119024 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
688566 195860 24 None 1 3 Rat 9.8 pKi = 9.8 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 337 4 1 4 2.6 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm00059a009
CHEMBL558910 195860 24 None 1 3 Rat 9.8 pKi = 9.8 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 337 4 1 4 2.6 O=C(O[C@H]1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1021/jm00059a009
10274019 204228 0 None -2 5 Human 9.8 pKi = 9.8 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 425 6 0 3 6.0 COc1ccc([S+]([O-])c2ccc(C(C)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL71124 204228 0 None -2 5 Human 9.8 pKi = 9.8 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 425 6 0 3 6.0 COc1ccc([S+]([O-])c2ccc(C(C)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
11431874 74251 0 None -1 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M3 receptor expressed in CHO cell membraneDisplacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M3 receptor expressed in CHO cell membrane
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2023762 74251 0 None -1 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M3 receptor expressed in CHO cell membraneDisplacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M3 receptor expressed in CHO cell membrane
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL2023764 74251 0 None -1 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M3 receptor expressed in CHO cell membraneDisplacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M3 receptor expressed in CHO cell membrane
ChEMBL 413 9 0 1 6.6 C=CCCCC[N+]1(C)C2CCC1CC(CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
86765983 145789 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 342 4 0 2 4.1 C[C@@](C(=O)O[C@@H]1CC2CCC1[N+]2(C)C)(c1ccccc1)C1CCCC1 nan
CHEMBL3917058 145789 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 342 4 0 2 4.1 C[C@@](C(=O)O[C@@H]1CC2CCC1[N+]2(C)C)(c1ccccc1)C1CCCC1 nan
16065407 67915 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2F)C1 10.1021/jm200884j
CHEMBL1910865 67915 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 462 9 2 4 4.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2F)C1 10.1021/jm200884j
156015976 178298 0 None 2 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 337 3 1 2 4.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccccc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4644192 178298 0 None 2 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 337 3 1 2 4.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccccc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4651109 178298 0 None 2 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 337 3 1 2 4.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccccc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
16086001 139189 0 None 117 5 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 716 11 2 5 5.0 O=C(NCC1CCN(CC2CC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL378772 139189 0 None 117 5 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 716 11 2 5 5.0 O=C(NCC1CCN(CC2CC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
10326800 58511 1 None 70 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683938 58511 1 None 70 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
25897919 55622 14 None -2 8 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmc.2014.04.031
657309 55622 14 None -2 8 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmc.2014.04.031
CHEMBL1464005 55622 14 None -2 8 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmc.2014.04.031
CHEMBL1621597 55622 14 None -2 8 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmc.2014.04.031
16034837 67901 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910851 67901 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
53372934 129274 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670826 129274 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
53372936 129275 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670827 129275 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
59291413 112760 0 None -1 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.1 O=C(Nc1ccsc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298589 112760 0 None -1 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.1 O=C(Nc1ccsc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305767 112760 0 None -1 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.1 O=C(Nc1ccsc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
16086063 80533 0 None 57 5 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 744 11 2 5 5.8 O=C(NCC1CCN(CC2CCCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL214898 80533 0 None 57 5 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 744 11 2 5 5.8 O=C(NCC1CCN(CC2CCCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL5076266 214401 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(F)c(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5076445 214418 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CCN3C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5076558 214425 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2cccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5084383 214889 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3cccc(F)c3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5090464 215241 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)c1ccc(CN(C(=O)O[C@H]2CN3CCC2CC3)c2ccccc2F)s1 10.1021/acs.jmedchem.1c00204
168290830 191931 0 None -7 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 790 17 5 11 6.0 COc1cc(C(=O)OCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
CHEMBL5200887 191931 0 None -7 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 790 17 5 11 6.0 COc1cc(C(=O)OCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
367 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
5487427 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
8592 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
CHEMBL1900528 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
CHEMBL3305968 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
CHEMBL4650755 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
DB01409 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmcl.2008.03.024
10269503 167056 0 None 7 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#C[C@](O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL428962 167056 0 None 7 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#C[C@](O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
10327462 119021 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl 10.1021/jm501915g
CHEMBL3426688 119021 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl 10.1021/jm501915g
10327461 119023 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c(Cl)c1 10.1021/jm501915g
CHEMBL3426690 119023 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c(Cl)c1 10.1021/jm501915g
118737357 119038 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 703 12 5 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426705 119038 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 703 12 5 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
44406573 72945 0 None 6 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#CC(O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200693 72945 0 None 6 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#CC(O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
59291259 112446 1 None 1 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.6 O=C(Nc1ncsc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298591 112446 1 None 1 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.6 O=C(Nc1ncsc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
367 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
5487427 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
8592 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
CHEMBL1900528 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
CHEMBL3305968 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
CHEMBL4650755 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
DB01409 3795 12 None 2 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2019.06.016
59548051 125193 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645292 125193 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548124 125195 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645294 125195 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548120 125197 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645296 125197 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548119 125200 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645299 125200 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548129 125203 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645301 125203 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843902 125204 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645302 125204 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548098 125205 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645303 125205 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548123 125206 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645304 125206 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548095 125209 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645307 125209 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548136 125212 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645310 125212 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843740 125214 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645312 125214 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843734 125218 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645316 125218 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548091 125219 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645317 125219 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548077 125221 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645319 125221 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548132 125223 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645320 125223 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548118 125224 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645321 125224 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548139 125226 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645323 125226 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548058 125234 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645331 125234 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548052 125240 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645337 125240 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548072 125242 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645339 125242 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548114 125248 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645344 125248 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548116 125251 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645347 125251 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548085 125253 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645349 125253 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548078 125257 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645353 125257 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548082 125258 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645354 125258 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548137 125261 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645357 125261 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548105 125265 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645361 125265 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
118405900 153644 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 852 15 6 10 7.4 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3981221 153644 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 852 15 6 10 7.4 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548051 125193 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645292 125193 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548124 125195 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645294 125195 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548120 125197 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645296 125197 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548087 125198 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 872 15 6 10 7.7 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645297 125198 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 872 15 6 10 7.7 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548119 125200 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645299 125200 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548129 125203 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645301 125203 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843902 125204 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645302 125204 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548098 125205 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645303 125205 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548123 125206 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645304 125206 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548095 125209 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645307 125209 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548136 125212 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645310 125212 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843740 125214 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645312 125214 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843734 125218 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645316 125218 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548091 125219 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645317 125219 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548077 125221 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645319 125221 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548132 125223 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645320 125223 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548118 125224 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645321 125224 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548139 125226 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645323 125226 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548058 125234 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645331 125234 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548052 125240 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645337 125240 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548072 125242 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645339 125242 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548114 125248 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645344 125248 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548116 125251 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645347 125251 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548085 125253 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645349 125253 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548115 125254 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645350 125254 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548078 125257 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645353 125257 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548082 125258 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645354 125258 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548137 125261 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645357 125261 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548105 125265 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645361 125265 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548051 125193 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645292 125193 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548124 125195 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645294 125195 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548120 125197 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645296 125197 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548087 125198 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 872 15 6 10 7.7 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645297 125198 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 872 15 6 10 7.7 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548119 125200 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645299 125200 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548129 125203 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645301 125203 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843902 125204 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645302 125204 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548098 125205 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645303 125205 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548123 125206 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645304 125206 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548095 125209 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645307 125209 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548136 125212 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645310 125212 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843740 125214 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645312 125214 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843734 125218 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645316 125218 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548091 125219 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645317 125219 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548077 125221 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645319 125221 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548132 125223 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645320 125223 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548118 125224 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645321 125224 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548139 125226 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645323 125226 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548058 125234 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645331 125234 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548052 125240 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645337 125240 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548072 125242 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645339 125242 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548114 125248 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645344 125248 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548116 125251 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645347 125251 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548085 125253 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645349 125253 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548115 125254 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645350 125254 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548078 125257 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645353 125257 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548082 125258 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645354 125258 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548137 125261 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645357 125261 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548105 125265 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645361 125265 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
16065137 67900 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
CHEMBL1910850 67900 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 458 9 2 4 4.9 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2cccc(O)c2)C1 10.1021/jm200884j
59291461 112748 0 None 2 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1cscc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298334 112748 0 None 2 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1cscc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305613 112748 0 None 2 3 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.2 O=C(Nc1cscc1-c1ccccc1)OC12CCN(CC1)CC2 10.1016/j.bmc.2014.04.031
25897919 55622 14 None 1 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
657309 55622 14 None 1 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
CHEMBL1464005 55622 14 None 1 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
CHEMBL1621597 55622 14 None 1 8 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 24 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
44431393 87995 0 None -1 3 Human 9.7 pKi = 9.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 402 6 1 5 3.5 CN(C)C1(CNCCC2CCOCC2)COc2cc(Cl)c(Cl)cc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234440 87995 0 None -1 3 Human 9.7 pKi = 9.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 402 6 1 5 3.5 CN(C)C1(CNCCC2CCOCC2)COc2cc(Cl)c(Cl)cc2OC1 10.1016/j.bmcl.2006.11.058
1734 116 10 None 1 13 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
307 116 10 None 1 13 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
CHEMBL168067 116 10 None 1 13 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/acs.jmedchem.6b01422
53372938 129276 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670828 129276 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
138680032 178278 0 None 3 3 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 355 3 1 2 4.3 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4639307 178278 0 None 3 3 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 355 3 1 2 4.3 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650981 178278 0 None 3 3 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 355 3 1 2 4.3 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
49800047 14451 1 None -2 5 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
CHEMBL1201024 14451 1 None -2 5 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
CHEMBL1201268 14451 1 None -2 5 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
10919522 78889 0 None 3 5 Human 9.6 pKi = 9.6 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 688 11 1 4 6.8 O=C(NC[C@H]1CCCN(CC2CCCCC2)C1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm010480k
CHEMBL2112957 78889 0 None 3 5 Human 9.6 pKi = 9.6 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 688 11 1 4 6.8 O=C(NC[C@H]1CCCN(CC2CCCCC2)C1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm010480k
9946298 72798 0 None 3 2 Human 9.6 pKi = 9.6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 CO[C@]1(C#C[C@@](O)(c2ccccc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200171 72798 0 None 3 2 Human 9.6 pKi = 9.6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 CO[C@]1(C#C[C@@](O)(c2ccccc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44406597 72880 0 None 12 2 Human 9.6 pKi = 9.6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 339 3 1 3 3.2 COC1(C#CC(O)(c2ccccc2)C2CCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200432 72880 0 None 12 2 Human 9.6 pKi = 9.6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 339 3 1 3 3.2 COC1(C#CC(O)(c2ccccc2)C2CCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
59291513 112791 0 None 1 3 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 378 3 1 4 4.3 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ncsc1-c1cccc(Cl)c1)C2 10.1016/j.bmc.2014.04.031
CHEMBL3298598 112791 0 None 1 3 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 378 3 1 4 4.3 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ncsc1-c1cccc(Cl)c1)C2 10.1016/j.bmc.2014.04.031
CHEMBL3307127 112791 0 None 1 3 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 378 3 1 4 4.3 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ncsc1-c1cccc(Cl)c1)C2 10.1016/j.bmc.2014.04.031
138710679 178151 0 None 2 3 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 396 4 2 3 5.3 O=C(Nc1ccc(F)cc1-c1ccc(Cl)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4649201 178151 0 None 2 3 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 396 4 2 3 5.3 O=C(Nc1ccc(F)cc1-c1ccc(Cl)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL5086393 215003 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5090179 215224 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1cc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3F)s2)ccc1OC(F)F 10.1021/acs.jmedchem.1c00204
71113213 184425 0 None -1 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 696 18 5 8 6.6 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4846536 184425 0 None -1 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 696 18 5 8 6.6 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164621790 185768 0 None -5 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 849 17 5 9 7.6 CCN(CCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C(=O)c1ccc(COc2cccc(-c3ccc([C@@H](NC(=O)O[C@H]4CN5CCC4CC5)c4ccccc4)cc3)c2)cc1 10.1016/j.bmcl.2021.127975
CHEMBL4866806 185768 0 None -5 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 849 17 5 9 7.6 CCN(CCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C(=O)c1ccc(COc2cccc(-c3ccc([C@@H](NC(=O)O[C@H]4CN5CCC4CC5)c4ccccc4)cc3)c2)cc1 10.1016/j.bmcl.2021.127975
154417 93231 60 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2013.12.024
CHEMBL2449003 93231 60 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2013.12.024
127044 78881 1 None 2 3 Rat 9.6 pKi = 9.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 427 5 1 4 2.9 O=C(OC1CN2CCC1CC2)C(O)(CC=CI)c1ccccc1 10.1021/jm00059a009
CHEMBL2112942 78881 1 None 2 3 Rat 9.6 pKi = 9.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 427 5 1 4 2.9 O=C(OC1CN2CCC1CC2)C(O)(CC=CI)c1ccccc1 10.1021/jm00059a009
154417 93231 60 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2013.12.024
CHEMBL2449003 93231 60 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2013.12.024
1201549 594 24 None -1 20 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 594 24 None -1 20 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 594 24 None -1 20 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 594 24 None -1 20 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 594 24 None -1 20 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 594 24 None -1 20 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
54580129 61765 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 786 21 6 8 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773197 61765 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 786 21 6 8 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL5284000 194216 0 None 1 3 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 493 11 2 4 6.6 NCCCCCCCCN1CCC(OC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c01376
25897919 55622 14 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
657309 55622 14 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
CHEMBL1464005 55622 14 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
CHEMBL1621597 55622 14 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm200884j
44610056 123965 0 None -2 5 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 704 14 5 9 5.5 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc([C@](O)(c6ccccc6)C6CCCCC6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629360 123965 0 None -2 5 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 704 14 5 9 5.5 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc([C@](O)(c6ccccc6)C6CCCCC6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
16086059 80746 0 None -1 7 Human 9.5 pKi = 9.5 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm301774u
CHEMBL215180 80746 0 None -1 7 Human 9.5 pKi = 9.5 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm301774u
367 3795 12 None -27 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
5487427 3795 12 None -27 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
8592 3795 12 None -27 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
CHEMBL1900528 3795 12 None -27 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
CHEMBL3305968 3795 12 None -27 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
CHEMBL4650755 3795 12 None -27 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
DB01409 3795 12 None -27 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1016/j.bmc.2014.04.031
16086059 80746 0 None -1 7 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL215180 80746 0 None -1 7 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
70843738 125215 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645313 125215 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548128 125232 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645329 125232 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548080 125237 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645334 125237 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548088 125241 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645338 125241 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548059 125244 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645340 125244 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548084 125246 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645342 125246 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
118405092 150229 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 848 15 5 8 8.9 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](C)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3952427 150229 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 848 15 5 8 8.9 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](C)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548106 125208 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645306 125208 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843738 125215 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645313 125215 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548128 125232 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645329 125232 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548080 125237 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645334 125237 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548088 125241 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645338 125241 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548059 125244 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645340 125244 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548084 125246 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645342 125246 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548106 125208 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645306 125208 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
70843738 125215 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645313 125215 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548128 125232 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645329 125232 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548080 125237 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645334 125237 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548088 125241 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645338 125241 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548059 125244 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645340 125244 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548084 125246 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645342 125246 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
53239456 61788 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773267 61788 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
11039424 78887 1 None 45 5 Human 9.5 pKi = 9.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 622 14 3 4 5.4 O=C(CCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112955 78887 1 None 45 5 Human 9.5 pKi = 9.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 622 14 3 4 5.4 O=C(CCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
53239456 61788 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2015.10.008
CHEMBL1773267 61788 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2015.10.008
72712268 106431 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 406 5 1 6 2.4 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(CO)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3091670 106431 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 406 5 1 6 2.4 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(CO)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3140032 106431 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 406 5 1 6 2.4 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(CO)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL5076680 214435 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)Cc2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)cc2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5081816 214747 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5084829 214914 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None CCOc1cc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3F)s2)ccc1OC(F)F 10.1021/acs.jmedchem.1c00204
CHEMBL5085717 214961 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None CC(C)Oc1cc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3F)s2)ccc1OC(F)F 10.1021/acs.jmedchem.1c00204
CHEMBL5086769 215025 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3cccc(O)c3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5088742 215152 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2cccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
71113309 185557 0 None -19 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 654 15 5 8 5.4 O=C(NC(c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4863525 185557 0 None -19 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 654 15 5 8 5.4 O=C(NC(c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
71093373 192400 0 None -7 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(NC(c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5208201 192400 0 None -7 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(NC(c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
25897919 55622 14 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2008.03.024
657309 55622 14 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2008.03.024
CHEMBL1464005 55622 14 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2008.03.024
CHEMBL1621597 55622 14 None 1 8 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1016/j.bmcl.2008.03.024
25010559 96740 0 None 10 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 381 3 1 3 4.3 CO[C@]1(C#C[C@](O)(c2ccccc2)C2CCCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL264676 96740 0 None 10 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 381 3 1 3 4.3 CO[C@]1(C#C[C@](O)(c2ccccc2)C2CCCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
10109563 158516 0 None 7 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 367 3 1 3 4.0 CO[C@]1(C#C[C@](O)(c2ccccc2)C2CCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL409151 158516 0 None 7 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 367 3 1 3 4.0 CO[C@]1(C#C[C@](O)(c2ccccc2)C2CCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
118737352 119029 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 13 6 9 6.1 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426696 119029 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 13 6 9 6.1 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
10394806 119031 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 681 12 6 8 5.3 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)N[C@H]1CC[C@H](CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
CHEMBL3426698 119031 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 681 12 6 8 5.3 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)N[C@H]1CC[C@H](CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
118737356 119036 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 753 13 5 9 6.5 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426703 119036 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 753 13 5 9 6.5 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
16086059 80746 0 None -1 7 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL215180 80746 0 None -1 7 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
44406662 166259 0 None 12 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 366 3 1 4 2.6 COC1(C#CC(O)(c2ccccc2)c2ccc(F)nc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL427013 166259 0 None 12 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 366 3 1 4 2.6 COC1(C#CC(O)(c2ccccc2)c2ccc(F)nc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
9986442 58507 0 None 10 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 626 15 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683933 58507 0 None 10 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 626 15 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL5265833 193433 0 None 1 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 488 10 1 3 7.1 C#CCCCCCCN1CCC(COC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c01376
16116085 11814 0 None -3 5 Human 9.5 pKi = 9.5 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1182201 11814 0 None -3 5 Human 9.5 pKi = 9.5 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL219786 11814 0 None -3 5 Human 9.5 pKi = 9.5 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
122194236 123959 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 362 5 1 5 2.9 CN1CCC(Cn2cnc(C(O)(c3ccccc3)c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.10.008
CHEMBL3629354 123959 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 362 5 1 5 2.9 CN1CCC(Cn2cnc(C(O)(c3ccccc3)c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.10.008
155157200 177914 0 None 1 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 340 3 1 3 4.1 O=C(Nc1ccc(F)cc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4645543 177914 0 None 1 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 340 3 1 3 4.1 O=C(Nc1ccc(F)cc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
156015097 177528 0 None 1 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4640324 177528 0 None 1 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
10567858 177855 0 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 322 3 1 3 4.0 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4644670 177855 0 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 322 3 1 3 4.0 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
59291327 112790 0 None -1 3 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 344 3 1 4 3.6 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ncsc1-c1ccccc1)C2 10.1016/j.bmc.2014.04.031
CHEMBL3298597 112790 0 None -1 3 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 344 3 1 4 3.6 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ncsc1-c1ccccc1)C2 10.1016/j.bmc.2014.04.031
CHEMBL3307126 112790 0 None -1 3 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 344 3 1 4 3.6 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ncsc1-c1ccccc1)C2 10.1016/j.bmc.2014.04.031
71454563 79627 0 None -6 4 Human 9.4 pKi = 9.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 423 6 0 3 5.9 C=C(c1ccc([S@+]([O-])c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
CHEMBL2115128 79627 0 None -6 4 Human 9.4 pKi = 9.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 423 6 0 3 5.9 C=C(c1ccc([S@+]([O-])c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
90666101 109305 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 666 18 5 8 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219031 109305 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 666 18 5 8 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1039/C1MD00140J
156021744 178090 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4648071 178090 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
16086066 139210 0 None 134 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 710 9 3 5 5.4 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
CHEMBL378872 139210 0 None 134 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 710 9 3 5 5.4 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
16086060 168919 0 None 100 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL438822 168919 0 None 100 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 662 9 3 5 3.9 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
54583092 61766 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 695 19 6 7 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(C[C@@H](C)NC[C@H](O)c3cc(O)cc(O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773198 61766 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 695 19 6 7 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(C[C@@H](C)NC[C@H](O)c3cc(O)cc(O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL5076535 214422 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCCN(C)C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5076558 214425 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2cccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5087564 215085 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2cccc(NC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
164616287 184972 0 None -3 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 668 16 5 8 5.8 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4854418 184972 0 None -3 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 668 16 5 8 5.8 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164627621 186302 0 None -15 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 640 14 5 8 5.0 O=C(NC(c1ccccc1)c1cccc(OCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4874819 186302 0 None -15 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 640 14 5 8 5.0 O=C(NC(c1ccccc1)c1cccc(OCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
44406481 72846 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 COC1(C#CC(O)(c2ccccc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200319 72846 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 COC1(C#CC(O)(c2ccccc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
1734 116 10 None 1 13 Human 9.4 pKi = 9.4 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
307 116 10 None 1 13 Human 9.4 pKi = 9.4 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
CHEMBL168067 116 10 None 1 13 Human 9.4 pKi = 9.4 Binding
Binding affinity to human muscarinic M3 receptor by radioligand displacement assayBinding affinity to human muscarinic M3 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
134272501 176557 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4483083 176557 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597500 176557 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(O[C@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
70843737 125217 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645315 125217 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548060 125239 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645336 125239 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843737 125217 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645315 125217 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548060 125239 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645336 125239 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843737 125217 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645315 125217 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548060 125239 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645336 125239 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
1734 116 10 None 1 13 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
307 116 10 None 1 13 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
CHEMBL168067 116 10 None 1 13 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M3 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M3 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
174174 521 49 None -2 14 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
260 521 49 None -2 14 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
320 521 49 None -2 14 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
CHEMBL517712 521 49 None -2 14 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
DB00572 521 49 None -2 14 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
1734 116 10 None 1 13 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm401895u
307 116 10 None 1 13 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm401895u
CHEMBL168067 116 10 None 1 13 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm401895u
134272452 176650 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(OC1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4448944 176650 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(OC1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4598232 176650 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(OC1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
11223598 106498 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3084413 106498 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
CHEMBL3140264 106498 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 330 3 0 2 5.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](C=C(c1cccs1)c1cccs1)C2 10.1021/jm900736e
11061341 78890 0 None 23 5 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 662 13 2 4 6.3 O=C(CCNC(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112958 78890 0 None 23 5 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 662 13 2 4 6.3 O=C(CCNC(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
10567858 177855 0 None -1 6 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptorDisplacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptor
ChEMBL 322 3 1 3 4.0 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4644670 177855 0 None -1 6 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptorDisplacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptor
ChEMBL 322 3 1 3 4.0 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
156013794 177252 0 None 3 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 310 4 2 3 3.9 O=C(Nc1ccccc1-c1ccccc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636302 177252 0 None 3 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 310 4 2 3 3.9 O=C(Nc1ccccc1-c1ccccc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
15599352 108596 0 None -2 2 Rat 9.3 pKi = 9.3 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL320611 108596 0 None -2 2 Rat 9.3 pKi = 9.3 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
9867847 204235 0 None -2 4 Human 9.3 pKi = 9.3 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 439 6 0 4 5.6 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
CHEMBL71147 204235 0 None -2 4 Human 9.3 pKi = 9.3 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 439 6 0 4 5.6 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00437-6
9867847 204235 0 None -2 4 Human 9.3 pKi = 9.3 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 439 6 0 4 5.6 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00457-1
CHEMBL71147 204235 0 None -2 4 Human 9.3 pKi = 9.3 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 439 6 0 4 5.6 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCCCC2)CC1 10.1016/s0960-894x(00)00457-1
16085999 80263 0 None 60 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 676 10 3 5 4.3 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL214029 80263 0 None 60 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 676 10 3 5 4.3 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
174174 521 49 None -2 14 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
260 521 49 None -2 14 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
320 521 49 None -2 14 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
CHEMBL517712 521 49 None -2 14 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
DB00572 521 49 None -2 14 Human 9.3 pKi = 9.3 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm010480k
CHEMBL5076886 214444 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3C[C@H]4CC[C@H](C3)N4C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5078006 214505 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5085166 214930 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3ccccn3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
118737351 119028 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 13 6 9 6.1 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1C 10.1021/jm501915g
CHEMBL3426695 119028 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 13 6 9 6.1 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1C 10.1021/jm501915g
140844407 176608 0 None -4 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 490 8 1 3 5.4 O=C(OC1C[N+]2(CCCc3ccc(Cl)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4519930 176608 0 None -4 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 490 8 1 3 5.4 O=C(OC1C[N+]2(CCCc3ccc(Cl)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597916 176608 0 None -4 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 490 8 1 3 5.4 O=C(OC1C[N+]2(CCCc3ccc(Cl)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
16086064 79931 0 None 93 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 730 10 2 5 5.6 O=C(NCC1CCN(C2CCCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL212645 79931 0 None 93 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 730 10 2 5 5.6 O=C(NCC1CCN(C2CCCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
16086000 80327 0 None 79 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 676 9 2 5 4.2 CN1CCC(CNC(=O)[C@H]2CCCN2C(=O)[C@@H]2C[C@@H](O)CN2C(=O)CC(c2ccc(F)cc2)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm051205r
CHEMBL214342 80327 0 None 79 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 676 9 2 5 4.2 CN1CCC(CNC(=O)[C@H]2CCCN2C(=O)[C@@H]2C[C@@H](O)CN2C(=O)CC(c2ccc(F)cc2)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm051205r
71450948 79507 0 None -1 2 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1C[C@H]2OC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00090a006
CHEMBL2114060 79507 0 None -1 2 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1C[C@H]2OC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00090a006
53317170 58499 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 409 10 2 4 5.3 NCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683925 58499 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 409 10 2 4 5.3 NCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
138711343 177800 0 None 1 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 408 3 1 3 5.4 O=C(Nc1ccc(F)cc1-c1ccc(Cl)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4643867 177800 0 None 1 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 408 3 1 3 5.4 O=C(Nc1ccc(F)cc1-c1ccc(Cl)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
174174 521 49 None -2 14 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2018.12.022
260 521 49 None -2 14 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2018.12.022
320 521 49 None -2 14 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2018.12.022
CHEMBL517712 521 49 None -2 14 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2018.12.022
DB00572 521 49 None -2 14 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmcl.2018.12.022
16086062 80762 0 None 58 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 730 11 2 5 5.4 O=C(NCC1CCN(CC2CCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL215189 80762 0 None 58 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 730 11 2 5 5.4 O=C(NCC1CCN(CC2CCC2)CC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
71449175 79623 0 None 1 2 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1C[C@@H]2OC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00090a006
CHEMBL2115124 79623 0 None 1 2 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1C[C@@H]2OC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00090a006
3028236 102572 1 None 36 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 340 9 0 2 4.2 CC[N+](CC)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2377383 102572 1 None 36 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 340 9 0 2 4.2 CC[N+](CC)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL3041159 102572 1 None 36 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 340 9 0 2 4.2 CC[N+](CC)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
11434515 261 6 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmc.2019.06.016
11519741 261 6 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmc.2019.06.016
4484 261 6 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmc.2019.06.016
7449 261 6 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmc.2019.06.016
CHEMBL1194325 261 6 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmc.2019.06.016
DB08897 261 6 None -4 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmc.2019.06.016
2028 2958 80 None 1 11 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
359 2958 80 None 1 11 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
4634 2958 80 None 1 11 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
CHEMBL1231 2958 80 None 1 11 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
DB01062 2958 80 None 1 11 Human 9.2 pKi = 9.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC nan
16115945 12265 0 None -2 5 Human 9.2 pKi = 9.2 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1184886 12265 0 None -2 5 Human 9.2 pKi = 9.2 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL376057 12265 0 None -2 5 Human 9.2 pKi = 9.2 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL5289667 194452 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 959 21 2 5 13.8 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCCCN3CCC(OC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
9880462 72875 0 None 39 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 327 5 1 3 3.2 CCCCC(O)(C#CC1(OC)CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2005.09.079
CHEMBL200416 72875 0 None 39 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 327 5 1 3 3.2 CCCCC(O)(C#CC1(OC)CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2005.09.079
138711325 177872 0 None 3 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 328 4 2 3 4.0 O=C(Nc1ccc(F)cc1-c1ccccc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4644852 177872 0 None 3 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 328 4 2 3 4.0 O=C(Nc1ccc(F)cc1-c1ccccc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL5077424 214475 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C)C(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5086895 215031 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)c1cccc(CNC(C(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.1c00204
CHEMBL5094110 215448 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2cccc(S(=O)(=O)NC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1OC 10.1021/acs.jmedchem.1c00204
118737349 119025 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 739 13 6 9 6.4 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1Cl 10.1021/jm501915g
CHEMBL3426692 119025 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 739 13 6 9 6.4 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1Cl 10.1021/jm501915g
10439505 119032 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 675 12 6 8 5.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCNC(=O)c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)CC1 10.1021/jm501915g
CHEMBL3426699 119032 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 675 12 6 8 5.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCNC(=O)c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)CC1 10.1021/jm501915g
87142783 119037 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426704 119037 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
54583100 61785 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 731 21 5 8 7.4 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773264 61785 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 731 21 5 8 7.4 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
155619955 177501 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 368 3 1 4 3.7 CN1[C@H]2C[C@@H](OC(=O)Nc3ccc(F)cc3-c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/acs.jmedchem.0c00297
CHEMBL4639938 177501 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 368 3 1 4 3.7 CN1[C@H]2C[C@@H](OC(=O)Nc3ccc(F)cc3-c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/acs.jmedchem.0c00297
134272442 176464 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 4 4.9 O=C(OC1C[N+]2(CCSc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4457734 176464 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 4 4.9 O=C(OC1C[N+]2(CCSc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596671 176464 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 4 4.9 O=C(OC1C[N+]2(CCSc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
44420795 11818 0 None 7 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 426 6 1 1 4.4 C[N+]1(CCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL1182222 11818 0 None 7 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 426 6 1 1 4.4 C[N+]1(CCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL223055 11818 0 None 7 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 426 6 1 1 4.4 C[N+]1(CCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
1734 116 10 None 1 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2007.09.003
307 116 10 None 1 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2007.09.003
CHEMBL168067 116 10 None 1 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2007.09.003
16125331 136937 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 440 7 1 1 4.8 C[N+]1(CCCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL374452 136937 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 440 7 1 1 4.8 C[N+]1(CCCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
24764458 109315 3 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 716 18 6 9 6.9 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219042 109315 3 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 716 18 6 9 6.9 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
122194235 123958 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 690 16 6 8 7.3 O=C(Nc1ccccc1-c1ccc(O)c(Cl)c1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2015.10.008
CHEMBL3629353 123958 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 690 16 6 8 7.3 O=C(Nc1ccccc1-c1ccc(O)c(Cl)c1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2015.10.008
10438748 58506 0 None 13 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 612 14 5 7 6.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683932 58506 0 None 13 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 612 14 5 7 6.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
319 1312 44 None 2 9 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
321 1312 44 None 2 9 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031 1312 44 None 2 9 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
784 1312 44 None 2 9 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
CHEMBL1346 1312 44 None 2 9 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
DB00496 1312 44 None 2 9 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
16116083 12264 0 None -2 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL1184884 12264 0 None -2 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL375969 12264 0 None -2 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
53323772 58501 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 437 12 2 4 6.1 NCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683927 58501 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 437 12 2 4 6.1 NCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
16664965 84873 0 None 28 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 462 6 1 1 4.7 C[N+]1(CCc2ccccc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
CHEMBL223668 84873 0 None 28 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 462 6 1 1 4.7 C[N+]1(CCc2ccccc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
11828362 78891 0 None 39 5 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 636 15 3 4 5.8 O=C(CCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112959 78891 0 None 39 5 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 636 15 3 4 5.8 O=C(CCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
24876564 61751 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 668 20 5 7 7.5 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773074 61751 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 668 20 5 7 7.5 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL5279174 193992 0 None 1 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 474 9 1 3 6.7 C#CCCCCCN1CCC(COC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c01376
2028 2958 80 None 1 11 Human 9.1 pKi = 9.1 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2006.11.058
359 2958 80 None 1 11 Human 9.1 pKi = 9.1 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2006.11.058
4634 2958 80 None 1 11 Human 9.1 pKi = 9.1 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2006.11.058
CHEMBL1231 2958 80 None 1 11 Human 9.1 pKi = 9.1 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2006.11.058
DB01062 2958 80 None 1 11 Human 9.1 pKi = 9.1 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2006.11.058
44406686 140886 0 None 3 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 366 3 1 4 2.6 COC1(C#CC(O)(c2ccccc2)c2cccnc2F)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL382213 140886 0 None 3 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 366 3 1 4 2.6 COC1(C#CC(O)(c2ccccc2)c2cccnc2F)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
10199963 141290 0 None 6 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 383 3 1 3 3.3 CO[C@]1(C#CC(O)(c2cccc(F)c2)c2cccc(F)c2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL383389 141290 0 None 6 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 383 3 1 3 3.3 CO[C@]1(C#CC(O)(c2cccc(F)c2)c2cccc(F)c2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
25897919 55622 14 None 1 8 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/acs.jmedchem.1c00204
657309 55622 14 None 1 8 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/acs.jmedchem.1c00204
CHEMBL1464005 55622 14 None 1 8 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/acs.jmedchem.1c00204
CHEMBL1621597 55622 14 None 1 8 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/acs.jmedchem.1c00204
CHEMBL5078680 214556 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)c1cccc(NC(C(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.1c00204
CHEMBL5086272 214998 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3nccs3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
168279881 190838 0 None -15 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5184598 190838 0 None -15 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
86720814 191912 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 500 8 1 6 5.0 COC(=O)c1ccc(COc2cccc([C@@H](NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1 10.1021/acs.jmedchem.2c00609
CHEMBL5200448 191912 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 500 8 1 6 5.0 COC(=O)c1ccc(COc2cccc([C@@H](NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1 10.1021/acs.jmedchem.2c00609
118719922 115749 0 None 1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 115749 0 None 1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
118737355 119035 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 12 5 8 5.5 CN(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)C(=O)c1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
CHEMBL3426702 119035 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 12 5 8 5.5 CN(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)C(=O)c1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
44318782 206110 0 None 63 2 Human 9.1 pKi = 9.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 482 5 0 2 6.4 O=C(c1ccc(Cl)cc1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL85996 206110 0 None 63 2 Human 9.1 pKi = 9.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 482 5 0 2 6.4 O=C(c1ccc(Cl)cc1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
174174 521 49 None -1 14 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
260 521 49 None -1 14 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
320 521 49 None -1 14 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
CHEMBL517712 521 49 None -1 14 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
DB00572 521 49 None -1 14 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/nchembio.2007.55
59548053 125259 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645355 125259 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).Radioligand Binding Assay: Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM and eleven different test compound concentrations. The test compounds were initially dissolved to a concentration of 400 μM in dilution buffer and then serially diluted 5× with dilution buffer to final concentrations ranging from 10 pM to 100 μM. The order of addition and volumes added to the assay plates were as follows: 25 μL radioligand, 25 μL diluted test compound, and 50 μL membranes. Assay plates were incubated for 6 hours at 37° C. Binding reactions were terminated by rapid filtration over GF/B glass fiber filter plates (PerkinElmer, Inc.) pre-treated in 1% BSA. Filter plates were rinsed three times with wash buffer (10 mM HEPES) to remove unbound radioactivity. The plates were then air-dried and 50 μL Microscint-20 liquid scintillation fluid (PerkinElmer, Inc.) were added to each well. The plates were then counted in a PerkinElmer Topcount liquid scintillation counter (PerkinElmer, Inc.).
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548053 125259 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645355 125259 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.Radioligand Binding Assay: Radioligand binding assay using muscarinic receptors.
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548053 125259 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645355 125259 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.Radioligand Binding Assay: Radioligand binding assays for cloned muscarinic receptors were performed in 96-well microtiter plates in a total assay volume of 100 uL. CHO cell membranes stably expressing either the hM1, hM2, hM3, hM4 or hM5 muscarinic subtype were diluted in assay buffer to the following specific target protein concentrations (ug/well): 10 ug for hM1, 10-15 ug for hM2, 10-20 ug for hM3, 10-20 ug for hM4, and 10-12 ug for hM5 to get similar signals (cpm). The membranes were briefly homogenized using a Polytron tissue disruptor (10 seconds) prior to assay plate addition.Saturation binding studies for determining KD values of the radioligand were performed using L-[N-methyl-3H]scopolamine methyl chloride ([3H]-NMS) (TRK666, 84.0 Ci/mmol, Amersham Pharmacia Biotech, Buckinghamshire, England) at concentrations ranging from 0.001 nM to 20 nM.Displacement assays for determination of Ki values of test compounds were performed with [3H]-NMS at 1 nM.
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
11693 1814 16 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
3494 1814 16 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
4302 1814 16 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
7459 1814 16 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
CHEMBL1201335 1814 16 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
DB00986 1814 16 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
11155732 10515 17 None -2 3 Rat 9.1 pKi = 9.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@H]1c1ccccc1 10.1021/jm050099q
CHEMBL1169543 10515 17 None -2 3 Rat 9.1 pKi = 9.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@H]1c1ccccc1 10.1021/jm050099q
9874175 58508 1 None 34 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1039/C1MD00140J
CHEMBL1683934 58508 1 None 34 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1039/C1MD00140J
25897919 55622 14 None 1 8 Human 9.1 pKi = 9.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
657309 55622 14 None 1 8 Human 9.1 pKi = 9.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
CHEMBL1464005 55622 14 None 1 8 Human 9.1 pKi = 9.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
CHEMBL1621597 55622 14 None 1 8 Human 9.1 pKi = 9.1 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1021/jm900132z
319 1312 44 None 2 9 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
321 1312 44 None 2 9 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
444031 1312 44 None 2 9 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
784 1312 44 None 2 9 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
CHEMBL1346 1312 44 None 2 9 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
DB00496 1312 44 None 2 9 Human 9.1 pKi = 9.1 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm010480k
152278786 182728 1 None 1 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 1 hr by Radioligand binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 1 hr by Radioligand binding assay
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
CHEMBL4790083 182728 1 None 1 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 1 hr by Radioligand binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes assessed as inhibition constant incubated for 1 hr by Radioligand binding assay
ChEMBL 467 5 0 8 2.6 N#Cc1ccc(N2C3CCC2CN(C(=O)CCS(=O)(=O)c2cccc4ncsc24)C3)nc1 10.1021/acsmedchemlett.0c00626
75167447 178262 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4634230 178262 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650933 178262 0 None -1 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
134272561 176403 0 None 2 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 442 7 1 3 4.3 O=C(OC1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4540604 176403 0 None 2 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 442 7 1 3 4.3 O=C(OC1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596189 176403 0 None 2 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 442 7 1 3 4.3 O=C(OC1C[N+]2(CCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
145148382 176590 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 8 1 3 5.0 Cc1ccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)cc1 10.1016/j.bmc.2019.06.016
CHEMBL4590868 176590 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 8 1 3 5.0 Cc1ccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)cc1 10.1016/j.bmc.2019.06.016
CHEMBL4597793 176590 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 8 1 3 5.0 Cc1ccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)cc1 10.1016/j.bmc.2019.06.016
56667296 176617 0 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 472 9 1 4 4.5 O=C(OC1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4461243 176617 0 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 472 9 1 4 4.5 O=C(OC1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597972 176617 0 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 472 9 1 4 4.5 O=C(OC1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
16115951 141618 0 None 1 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL385328 141618 0 None 1 5 Human 9.1 pKi = 9.1 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
46188794 178295 0 None -2 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4645580 178295 0 None -2 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651099 178295 0 None -2 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
174174 521 49 None -2 14 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
260 521 49 None -2 14 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
320 521 49 None -2 14 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
CHEMBL517712 521 49 None -2 14 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
DB00572 521 49 None -2 14 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1021/jm100697g
156015287 177551 0 None 3 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 364 4 2 3 4.3 O=C(Nc1ccccc1-c1cc(F)c(F)c(F)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640544 177551 0 None 3 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 364 4 2 3 4.3 O=C(Nc1ccccc1-c1cc(F)c(F)c(F)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
16115947 11817 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1182214 11817 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL222259 11817 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
16086061 80189 0 None 99 5 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 690 10 2 5 4.6 CCN1CCC(CNC(=O)[C@H]2CCCN2C(=O)[C@@H]2C[C@@H](O)CN2C(=O)CC(c2ccc(F)cc2)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm051205r
CHEMBL213709 80189 0 None 99 5 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 690 10 2 5 4.6 CCN1CCC(CNC(=O)[C@H]2CCCN2C(=O)[C@@H]2C[C@@H](O)CN2C(=O)CC(c2ccc(F)cc2)(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm051205r
3042 1402 35 None -1 15 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1402 35 None -1 15 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1402 35 None -1 15 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1402 35 None -1 15 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1402 35 None -1 15 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
59291421 112750 0 None -1 3 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.5 O=C(Nc1ncsc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298592 112750 0 None -1 3 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.5 O=C(Nc1ncsc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305620 112750 0 None -1 3 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.5 O=C(Nc1ncsc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
2028 2958 80 None -1 11 Rat 9.0 pKi = 9.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.02.036
359 2958 80 None -1 11 Rat 9.0 pKi = 9.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.02.036
4634 2958 80 None -1 11 Rat 9.0 pKi = 9.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.02.036
CHEMBL1231 2958 80 None -1 11 Rat 9.0 pKi = 9.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.02.036
DB01062 2958 80 None -1 11 Rat 9.0 pKi = 9.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.02.036
156014269 177192 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4635500 177192 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
16125370 84617 0 None 2 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 1 2 5.0 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL222387 84617 0 None 2 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 1 2 5.0 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCCN(Cc2ccccc2)CC1 10.1021/jm061159a
154417 93231 60 None -3 9 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cells
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2007.12.051
CHEMBL2449003 93231 60 None -3 9 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cells
ChEMBL 289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2 10.1016/j.bmcl.2007.12.051
10180872 103102 0 None 1 4 Human 9.0 pKi = 9.0 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 426 6 0 4 4.9 COc1ccc([S+]([O-])c2ccc(C(C)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL307810 103102 0 None 1 4 Human 9.0 pKi = 9.0 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 426 6 0 4 4.9 COc1ccc([S+]([O-])c2ccc(C(C)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
54582151 61787 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 711 24 5 8 7.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773266 61787 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 711 24 5 8 7.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
11767229 78888 0 None 30 5 Human 9.0 pKi = 9 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 607 15 2 3 7.5 O=C(CCCCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112956 78888 0 None 30 5 Human 9.0 pKi = 9 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 607 15 2 3 7.5 O=C(CCCCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
44406598 72996 0 None 6 2 Human 9.0 pKi = 9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 3 1 3 2.8 COC1(C#CC(O)(c2ccccc2)C2CCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200957 72996 0 None 6 2 Human 9.0 pKi = 9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 3 1 3 2.8 COC1(C#CC(O)(c2ccccc2)C2CCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44406690 74964 0 None 1 2 Human 9.0 pKi = 9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 349 3 1 5 1.8 COC1(C#CC(O)(c2ccccc2)c2cncnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL203249 74964 0 None 1 2 Human 9.0 pKi = 9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 349 3 1 5 1.8 COC1(C#CC(O)(c2ccccc2)c2cncnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44406268 140771 0 None 19 2 Human 9.0 pKi = 9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 383 3 1 3 3.3 CO[C@]1(C#CC(O)(c2ccc(F)cc2)c2ccc(F)cc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL381878 140771 0 None 19 2 Human 9.0 pKi = 9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 383 3 1 3 3.3 CO[C@]1(C#CC(O)(c2ccc(F)cc2)c2ccc(F)cc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
90198269 190364 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 492 8 2 5 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OC[C@H]2CC[C@H](C(=O)O)CC2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5177499 190364 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 492 8 2 5 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OC[C@H]2CC[C@H](C(=O)O)CC2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5270925 193636 0 None -1 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 474 9 1 3 6.9 C#CCCCCCCN1CCC(OC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c01376
138711318 178096 0 None 4 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 346 4 2 3 4.2 O=C(Nc1ccc(F)cc1-c1ccc(F)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4648196 178096 0 None 4 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 346 4 2 3 4.2 O=C(Nc1ccc(F)cc1-c1ccc(F)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
118737358 119039 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 13 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1021/jm501915g
CHEMBL3426706 119039 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 13 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1021/jm501915g
10049361 206098 0 None 10 2 Human 9.0 pKi = 9 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 448 5 0 2 5.8 O=C(c1ccccc1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL85892 206098 0 None 10 2 Human 9.0 pKi = 9 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 448 5 0 2 5.8 O=C(c1ccccc1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
5284632 67372 13 None 1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b02100
CHEMBL1888176 67372 13 None 1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b02100
CHEMBL3084748 67372 13 None 1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b02100
16125642 141985 0 None 2 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 442 7 1 2 4.3 C[N+]1(CCOc2ccccc2)CC[C@@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL387546 141985 0 None 2 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 442 7 1 2 4.3 C[N+]1(CCOc2ccccc2)CC[C@@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
101882890 115750 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354069 115750 0 None -1 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 593 16 0 7 6.8 CN1CCC=C(c2nsnc2OCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
44308899 203983 0 None 1 3 Human 9.0 pKi = 9.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 330 5 2 3 2.7 NCCC1CCN(C(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL69648 203983 0 None 1 3 Human 9.0 pKi = 9.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 330 5 2 3 2.7 NCCC1CCN(C(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(03)00350-0
59707188 109319 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219046 109319 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
90666115 109321 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 702 17 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219048 109321 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 702 17 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
77157 34895 42 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 325 4 1 4 2.6 CN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2015.10.008
CHEMBL143228 34895 42 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 325 4 1 4 2.6 CN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2015.10.008
122194237 123960 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 368 5 1 5 3.4 CN1CCC(Cn2cnc(C(O)(c3ccccc3)C3CCCCC3)n2)CC1 10.1016/j.bmcl.2015.10.008
CHEMBL3629355 123960 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 368 5 1 5 3.4 CN1CCC(Cn2cnc(C(O)(c3ccccc3)C3CCCCC3)n2)CC1 10.1016/j.bmcl.2015.10.008
138710768 177789 0 None -1 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 354 3 1 3 4.7 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4643643 177789 0 None -1 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 354 3 1 3 4.7 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
155512178 176465 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 3 4.8 O=C(OC1C[N+]2(CCCc3cccc(F)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4436930 176465 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 3 4.8 O=C(OC1C[N+]2(CCCc3cccc(F)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596672 176465 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 3 4.8 O=C(OC1C[N+]2(CCCc3cccc(F)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
15599355 107519 0 None -5 2 Rat 9.0 pKi = 9.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 351 4 1 4 2.9 CN1CC2CC1C[C@@H](OC(=O)C(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL318812 107519 0 None -5 2 Rat 9.0 pKi = 9.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 351 4 1 4 2.9 CN1CC2CC1C[C@@H](OC(=O)C(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
1734 116 10 None -2 13 Rat 8.9 pKi = 8.9 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00403-G
307 116 10 None -2 13 Rat 8.9 pKi = 8.9 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00403-G
CHEMBL168067 116 10 None -2 13 Rat 8.9 pKi = 8.9 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00403-G
1734 116 10 None -2 13 Rat 8.9 pKi = 8.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00113-8
307 116 10 None -2 13 Rat 8.9 pKi = 8.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00113-8
CHEMBL168067 116 10 None -2 13 Rat 8.9 pKi = 8.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/0960-894X(95)00113-8
44308832 203790 0 None 1 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 364 4 2 3 2.8 NCC=C1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL68384 203790 0 None 1 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 364 4 2 3 2.8 NCC=C1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL5285607 194281 0 None -1 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1052 21 1 13 10.0 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
16086005 139206 0 None 19 5 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 724 10 3 5 5.8 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
CHEMBL378859 139206 0 None 19 5 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 724 10 3 5 5.8 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
CHEMBL5080391 214660 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)c1cccc(CN(C(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.1c00204
CHEMBL5081214 214710 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None O=C(O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)c1cccc(S(=O)(=O)NC(C(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.1c00204
59591029 185899 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 336 4 1 3 3.6 O=C(NC(c1ccccc1)c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4869096 185899 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 336 4 1 3 3.6 O=C(NC(c1ccccc1)c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
118737350 119027 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426694 119027 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
44319071 205996 0 None 7 2 Human 8.9 pKi = 8.9 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 404 5 0 2 5.7 O=C(c1ccccc1)N(c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL84993 205996 0 None 7 2 Human 8.9 pKi = 8.9 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 404 5 0 2 5.7 O=C(c1ccccc1)N(c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
319 1312 44 None 2 9 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2005.09.079
321 1312 44 None 2 9 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2005.09.079
444031 1312 44 None 2 9 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2005.09.079
784 1312 44 None 2 9 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2005.09.079
CHEMBL1346 1312 44 None 2 9 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2005.09.079
DB00496 1312 44 None 2 9 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2005.09.079
2028 2958 80 None 1 11 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.09.079
359 2958 80 None 1 11 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.09.079
4634 2958 80 None 1 11 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.09.079
CHEMBL1231 2958 80 None 1 11 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.09.079
DB01062 2958 80 None 1 11 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1016/j.bmcl.2005.09.079
44406521 73877 0 None 4 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 COC1(C#CC(O)(c2ccccc2)c2ccncc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL201933 73877 0 None 4 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 COC1(C#CC(O)(c2ccccc2)c2ccncc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
90666120 109327 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 728 19 6 9 6.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@@H]3[C@@H](COC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)[C@@H]3C2)ccc1O 10.1039/C1MD00140J
CHEMBL3219053 109327 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 728 19 6 9 6.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@@H]3[C@@H](COC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)[C@@H]3C2)ccc1O 10.1039/C1MD00140J
44430454 87925 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 300 3 0 4 3.6 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCCC1 10.1016/j.bmcl.2007.03.047
CHEMBL234099 87925 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 300 3 0 4 3.6 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCCC1 10.1016/j.bmcl.2007.03.047
15888011 204290 0 None -1 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 302 3 2 3 2.0 NC1CCN(C(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL71431 204290 0 None -1 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 302 3 2 3 2.0 NC1CCN(C(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(03)00350-0
16115799 83413 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL219825 83413 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
54586986 61784 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 780 27 6 8 8.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)CCCCCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773263 61784 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 780 27 6 8 8.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)CCCCCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
57326235 77156 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042405 77156 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079009 77156 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
44431384 148836 0 None -2 3 Human 8.8 pKi = 8.8 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 384 6 1 4 4.0 CN(C)C1(CNCCC23CC4CC(CC(C4)C2)C3)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL394137 148836 0 None -2 3 Human 8.8 pKi = 8.8 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 384 6 1 4 4.0 CN(C)C1(CNCCC23CC4CC(CC(C4)C2)C3)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
156018620 177882 0 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 396 4 2 3 5.3 O=C(Nc1ccc(F)cc1-c1cc(Cl)cc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4644999 177882 0 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 396 4 2 3 5.3 O=C(Nc1ccc(F)cc1-c1cc(Cl)cc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
155542840 176369 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 540 9 1 4 5.6 O=C(OC1C[N+]2(CCCc3ccc(OC(F)(F)F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4521993 176369 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 540 9 1 4 5.6 O=C(OC1C[N+]2(CCCc3ccc(OC(F)(F)F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4595947 176369 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 540 9 1 4 5.6 O=C(OC1C[N+]2(CCCc3ccc(OC(F)(F)F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
53372938 129276 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670828 129276 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
2028 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
359 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
4634 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
CHEMBL1231 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
DB01062 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm2013216
57326326 77149 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042553 77149 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078942 77149 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
44627858 14006 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197382 14006 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569307 14006 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
57326326 77149 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL2042553 77149 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL2078942 77149 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
72712276 106429 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 406 5 0 6 3.0 COC(C(=O)O[C@@H]1C[C@H]2[C@@H]3O[C@@H]3[C@@H](C1)[N+]2(C)C)(c1cccs1)c1cccs1 10.1021/jm401219y
CHEMBL3091666 106429 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 406 5 0 6 3.0 COC(C(=O)O[C@@H]1C[C@H]2[C@@H]3O[C@@H]3[C@@H](C1)[N+]2(C)C)(c1cccs1)c1cccs1 10.1021/jm401219y
CHEMBL3140016 106429 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 406 5 0 6 3.0 COC(C(=O)O[C@@H]1C[C@H]2[C@@H]3O[C@@H]3[C@@H](C1)[N+]2(C)C)(c1cccs1)c1cccs1 10.1021/jm401219y
71093073 191564 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 500 8 1 6 5.0 COC(=O)c1ccc(COc2cccc(C(NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1 10.1021/acs.jmedchem.2c00609
CHEMBL5195203 191564 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 500 8 1 6 5.0 COC(=O)c1ccc(COc2cccc(C(NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1 10.1021/acs.jmedchem.2c00609
10484922 119022 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426689 119022 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
44319009 106909 0 None 15 2 Human 8.8 pKi = 8.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 426 5 0 2 5.2 O=C(C1CCC1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL314831 106909 0 None 15 2 Human 8.8 pKi = 8.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 426 5 0 2 5.2 O=C(C1CCC1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
53326588 58502 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 451 13 2 4 6.4 NCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683928 58502 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 451 13 2 4 6.4 NCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
16086067 81288 0 None 63 5 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 710 9 3 5 5.4 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
CHEMBL215894 81288 0 None 63 5 Human 8.8 pKi = 8.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 710 9 3 5 5.4 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(Cl)cc1)(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1021/jm051205r
16125704 84635 0 None 54 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 482 6 1 3 4.4 C[N+]1(CC(=O)c2ccsc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222450 84635 0 None 54 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 482 6 1 3 4.4 C[N+]1(CC(=O)c2ccsc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
44627853 197658 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL571121 197658 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
16115798 137853 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL376255 137853 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
15157137 99867 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 317 7 0 3 4.0 CN(C)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL286008 99867 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 317 7 0 3 4.0 CN(C)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
44308861 203505 0 None 1 3 Human 8.8 pKi = 8.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 316 4 2 3 2.3 NCC1CCN(C(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL66400 203505 0 None 1 3 Human 8.8 pKi = 8.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 316 4 2 3 2.3 NCC1CCN(C(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(03)00350-0
156015047 178242 0 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 409 4 1 2 5.3 C[N+]1(C)CCC(COC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00297
CHEMBL4645235 178242 0 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 409 4 1 2 5.3 C[N+]1(C)CCC(COC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00297
CHEMBL4650768 178242 0 None -1 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 409 4 1 2 5.3 C[N+]1(C)CCC(COC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00297
155520948 176405 0 None -3 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 3 4.8 O=C(OC1C[N+]2(CCCc3ccc(F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4450188 176405 0 None -3 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 3 4.8 O=C(OC1C[N+]2(CCCc3ccc(F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596191 176405 0 None -3 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 474 8 1 3 4.8 O=C(OC1C[N+]2(CCCc3ccc(F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
16124706 137497 0 None 61 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 437 5 1 4 5.1 Cc1cccc(CN2CCC(N3CC(c4cccs4)(c4cccs4)NC3=O)CC2)c1 10.1021/jm061159a
CHEMBL375420 137497 0 None 61 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 437 5 1 4 5.1 Cc1cccc(CN2CCC(N3CC(c4cccs4)(c4cccs4)NC3=O)CC2)c1 10.1021/jm061159a
16125587 84734 0 None 5 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 456 8 1 2 4.6 C[N+]1(CCCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL223028 84734 0 None 5 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 456 8 1 2 4.6 C[N+]1(CCCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
13567081 11202 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 320 4 0 2 4.3 C[N+](C)(C)C[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1178839 11202 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 320 4 0 2 4.3 C[N+](C)(C)C[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL45454 11202 0 None -1 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 320 4 0 2 4.3 C[N+](C)(C)C[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
53325045 58500 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 423 11 2 4 5.7 NCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683926 58500 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 423 11 2 4 5.7 NCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
90645361 112789 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 412 3 1 4 4.8 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cccc(C(F)(F)F)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298601 112789 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 412 3 1 4 4.8 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cccc(C(F)(F)F)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
CHEMBL3307123 112789 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 412 3 1 4 4.8 C[N+]12CCC(OC(=O)Nc3ncsc3-c3cccc(C(F)(F)F)c3)(CC1)CC2 10.1016/j.bmc.2014.04.031
16065135 67896 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910846 67896 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@H](Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL5287315 194356 0 None 1 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 460 8 1 3 6.5 C#CCCCCCN1CCC(OC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c01376
44443730 94004 0 None 21 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 432 6 2 3 4.7 CC(c1ccccc1)N1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
CHEMBL248811 94004 0 None 21 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 432 6 2 3 4.7 CC(c1ccccc1)N1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
16125646 136946 0 None 50 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 476 6 1 2 4.3 C[N+]1(CC(=O)c2ccccc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
CHEMBL374513 136946 0 None 50 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 476 6 1 2 4.3 C[N+]1(CC(=O)c2ccccc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
16125589 84670 0 None 16 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 440 6 1 2 4.1 C[N+]1(CC(=O)c2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222636 84670 0 None 16 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 440 6 1 2 4.1 C[N+]1(CC(=O)c2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
16125541 137182 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 442 7 1 2 4.3 C[N+]1(CCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL374989 137182 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 442 7 1 2 4.3 C[N+]1(CCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
54757332 67895 0 None 7 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 414 9 1 3 4.4 NC(=O)C(CCCN1CC[C@H](Oc2ccccc2)C1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
CHEMBL1910845 67895 0 None 7 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 414 9 1 3 4.4 NC(=O)C(CCCN1CC[C@H](Oc2ccccc2)C1)(c1ccccc1)c1ccccc1 10.1021/jm200884j
11718536 137820 0 None 41 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 411 5 1 2 4.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL376000 137820 0 None 41 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 411 5 1 2 4.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
155530273 176327 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 8 1 3 5.0 Cc1cccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)c1 10.1016/j.bmc.2019.06.016
CHEMBL4463636 176327 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 8 1 3 5.0 Cc1cccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)c1 10.1016/j.bmc.2019.06.016
CHEMBL4595649 176327 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 8 1 3 5.0 Cc1cccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)c1 10.1016/j.bmc.2019.06.016
156020548 178154 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4649224 178154 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)CC1COCC(c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
72712476 106430 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 304 3 1 4 1.0 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3091668 106430 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 304 3 1 4 1.0 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3140031 106430 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 304 3 1 4 1.0 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)c3ccccc3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
66875589 103363 0 None -3 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084662 103363 0 None -3 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 321 4 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
10155850 96713 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 367 3 1 3 4.0 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL264414 96713 0 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 367 3 1 3 4.0 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
10372836 102370 39 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3039518 102370 39 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
118737360 119041 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426708 119041 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
10789183 104340 0 None 25 2 Human 8.7 pKi = 8.7 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 438 5 0 2 6.3 O=C(c1ccccc1)N(c1ccc(Cl)c(Cl)c1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL310132 104340 0 None 25 2 Human 8.7 pKi = 8.7 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 438 5 0 2 6.3 O=C(c1ccccc1)N(c1ccc(Cl)c(Cl)c1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
44319342 205695 0 None 31 2 Human 8.7 pKi = 8.7 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 454 5 0 3 5.8 O=C(c1cccs1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL82512 205695 0 None 31 2 Human 8.7 pKi = 8.7 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 454 5 0 3 5.8 O=C(c1cccs1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
154059 3610 51 None 1 8 Rat 8.0 pKi = 8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1021/jm050099q
2457 3610 51 None 1 8 Rat 8.0 pKi = 8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1021/jm050099q
7483 3610 51 None 1 8 Rat 8.0 pKi = 8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1021/jm050099q
CHEMBL1734 3610 51 None 1 8 Rat 8.0 pKi = 8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1021/jm050099q
DB01591 3610 51 None 1 8 Rat 8.0 pKi = 8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1021/jm050099q
44406480 72815 0 None 5 2 Human 8.0 pKi = 8 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 COC1(C#CC(O)(c2ccccc2)c2ccccn2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200210 72815 0 None 5 2 Human 8.0 pKi = 8 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 COC1(C#CC(O)(c2ccccc2)c2ccccn2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL5076886 214444 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3C[C@H]4CC[C@H](C3)N4C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5081816 214747 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5086393 215003 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
90666106 109310 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cccc(F)c3O)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219036 109310 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cccc(F)c3O)CC2)ccc1O 10.1039/C1MD00140J
71113107 186556 0 None -39 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 696 18 5 8 6.6 O=C(NC(c1ccccc1)c1ccc(OCCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4878395 186556 0 None -39 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 696 18 5 8 6.6 O=C(NC(c1ccccc1)c1ccc(OCCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
372625 101120 11 None -31 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL295388 101120 11 None -31 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
372625 101120 11 None -31 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in A9 cells by scintillation counting analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in A9 cells by scintillation counting analysis
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1039/d0md00137f
CHEMBL295388 101120 11 None -31 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in A9 cells by scintillation counting analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in A9 cells by scintillation counting analysis
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1039/d0md00137f
372625 101120 11 None -31 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in mouse A9L cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in mouse A9L cell membranes after 60 mins by scintillation counting method
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL295388 101120 11 None -31 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in mouse A9L cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in mouse A9L cell membranes after 60 mins by scintillation counting method
ChEMBL 462 9 1 4 5.1 CCN(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
168296296 192373 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 488 8 2 7 3.7 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cnc(C(=O)O)cn2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5207792 192373 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 488 8 2 7 3.7 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cnc(C(=O)O)cn2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
54757560 65958 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 327 3 2 5 3.0 Oc1cccc(F)c1-n1nc(OC2CCNCC2)c2ccccc21 10.1021/jm2007535
CHEMBL1836645 65958 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 327 3 2 5 3.0 Oc1cccc(F)c1-n1nc(OC2CCNCC2)c2ccccc21 10.1021/jm2007535
9969695 160864 0 None 15 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 361 4 0 3 3.7 COC(C#C[C@@]1(OC)CN2CCC1CC2)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.024
CHEMBL411514 160864 0 None 15 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 361 4 0 3 3.7 COC(C#C[C@@]1(OC)CN2CCC1CC2)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.024
118719923 115751 0 None -1 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 621 18 0 7 7.6 CN1CCC=C(c2nsnc2OCCCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354070 115751 0 None -1 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 621 18 0 7 7.6 CN1CCC=C(c2nsnc2OCCCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
10193005 77126 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 2 1 4 3.5 C1CCCN(c2nc(C3CC3)nc3c2CCCCN3)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL207816 77126 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 2 1 4 3.5 C1CCCN(c2nc(C3CC3)nc3c2CCCCN3)CC1 10.1016/j.bmcl.2006.01.006
44409944 77295 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2(C)CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL208335 77295 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2(C)CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
44311771 164208 0 None -34 3 Human 8.0 pKi = 8 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 546 9 0 6 4.5 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCN(S(=O)(=O)CCC)CC2)CC1 10.1016/s0960-894x(00)00457-1
CHEMBL421113 164208 0 None -34 3 Human 8.0 pKi = 8 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 546 9 0 6 4.5 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCN(S(=O)(=O)CCC)CC2)CC1 10.1016/s0960-894x(00)00457-1
44455198 97629 0 None -2 10 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 899 22 3 7 10.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2007.11.022
CHEMBL271108 97629 0 None -2 10 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 899 22 3 7 10.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2007.11.022
44455198 97629 0 None -2 10 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 899 22 3 7 10.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)ccc1O)C(C)C 10.1021/acs.jmedchem.8b00041
CHEMBL271108 97629 0 None -2 10 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 899 22 3 7 10.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6cccs6)n5[B-]4(F)F)C=C3)cc2)ccc1O)C(C)C 10.1021/acs.jmedchem.8b00041
10316726 11996 0 None -40 5 Rat 8.0 pKi = 8.0 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
CHEMBL1183364 11996 0 None -40 5 Rat 8.0 pKi = 8.0 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
CHEMBL292857 11996 0 None -40 5 Rat 8.0 pKi = 8.0 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
15599352 108596 0 None -2 2 Rat 8.0 pKi = 8.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL320611 108596 0 None -2 2 Rat 8.0 pKi = 8.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
44308809 204358 0 None -1 3 Human 7.0 pKi = 7 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 366 5 3 3 2.9 NCC1CCC(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL71799 204358 0 None -1 3 Human 7.0 pKi = 7 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 366 5 3 3 2.9 NCC1CCC(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
135398737 955 93 None -10 92 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 955 93 None -10 92 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 955 93 None -10 92 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 955 93 None -10 92 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 955 93 None -10 92 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
135398745 2893 112 None -27 66 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 2893 112 None -27 66 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 2893 112 None -27 66 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 2893 112 None -27 66 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
44406387 72814 0 None 5 2 Human 7.0 pKi = 7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 375 3 1 3 3.7 CO[C@]1(C#CC(O)(c2ccc(C)cc2)c2ccc(C)cc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200209 72814 0 None 5 2 Human 7.0 pKi = 7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 375 3 1 3 3.7 CO[C@]1(C#CC(O)(c2ccc(C)cc2)c2ccc(C)cc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44406451 72913 0 None 6 2 Human 7.0 pKi = 7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 385 2 1 3 3.8 CO[C@]1(C#CC(O)C2c3ccccc3C=Cc3ccccc32)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200566 72913 0 None 6 2 Human 7.0 pKi = 7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 385 2 1 3 3.8 CO[C@]1(C#CC(O)C2c3ccccc3C=Cc3ccccc32)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
129989 450 51 None -16 9 Human 7.0 pKi = 7 Binding
Binding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
8584 450 51 None -16 9 Human 7.0 pKi = 7 Binding
Binding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
CHEMBL43383 450 51 None -16 9 Human 7.0 pKi = 7 Binding
Binding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
4011 82379 49 None -14 24 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 82379 49 None -14 24 Human 7.0 pKi = 7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
155566290 176556 0 None -1318 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4582879 176556 0 None -1318 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4597498 176556 0 None -1318 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
44409772 76741 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 304 5 1 5 3.0 CCc1c(NC2CC2)nc(C2CC2)nc1N1CCSCC1 10.1016/j.bmcl.2006.01.006
CHEMBL206826 76741 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 304 5 1 5 3.0 CCc1c(NC2CC2)nc(C2CC2)nc1N1CCSCC1 10.1016/j.bmcl.2006.01.006
44409462 140417 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 340 4 1 4 4.0 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(C(F)(F)F)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL380926 140417 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 340 4 1 4 4.0 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(C(F)(F)F)CC1 10.1016/j.bmcl.2006.01.006
44409755 166329 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 258 4 1 4 2.8 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL427390 166329 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 258 4 1 4 2.8 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCC1 10.1016/j.bmcl.2006.01.006
42853213 104317 7 None 7 2 Human 7.0 pKi = 7 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 360 5 0 3 4.6 O=C(c1ccco1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL310016 104317 7 None 7 2 Human 7.0 pKi = 7 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 360 5 0 3 4.6 O=C(c1ccco1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
10468535 98101 1 None -1 3 Human 7.0 pKi = 7 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 273 0 0 1 4.2 c1ccc2c(c1)C(=C1CN3CCC1CC3)c1ccccc1-2 10.1016/S0960-894X(01)80824-6
CHEMBL273586 98101 1 None -1 3 Human 7.0 pKi = 7 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 273 0 0 1 4.2 c1ccc2c(c1)C(=C1CN3CCC1CC3)c1ccccc1-2 10.1016/S0960-894X(01)80824-6
10572657 40509 0 None 4 3 Human 7.0 pKi = 7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 393 6 2 4 3.2 O=C(NC1CCN(Cc2cccnc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL148328 40509 0 None 4 3 Human 7.0 pKi = 7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 393 6 2 4 3.2 O=C(NC1CCN(Cc2cccnc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
10160219 4898 0 None -100 5 Human 7.0 pKi = 7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 436 5 1 5 5.5 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
CHEMBL104693 4898 0 None -100 5 Human 7.0 pKi = 7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 436 5 1 5 5.5 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
44406424 72641 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 483 3 1 3 5.1 CO[C@]1(C#CC(O)(c2cccc(C(F)(F)F)c2)c2cccc(C(F)(F)F)c2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL199591 72641 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 483 3 1 3 5.1 CO[C@]1(C#CC(O)(c2cccc(C(F)(F)F)c2)c2cccc(C(F)(F)F)c2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
127041952 137975 0 None -39 5 Human 6.0 pKi = 6 Binding
Binding affinity to muscarinic M3 receptor (unknown origin)Binding affinity to muscarinic M3 receptor (unknown origin)
ChEMBL 467 7 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CCOC(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2015.12.081
CHEMBL3764557 137975 0 None -39 5 Human 6.0 pKi = 6 Binding
Binding affinity to muscarinic M3 receptor (unknown origin)Binding affinity to muscarinic M3 receptor (unknown origin)
ChEMBL 467 7 0 8 4.4 Cc1ncoc1-c1nnc(SCCCN2CCOC(c3ccc(C(F)(F)F)cc3)C2)n1C 10.1016/j.bmcl.2015.12.081
3013847 188891 1 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 741 23 5 10 5.8 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
CHEMBL507760 188891 1 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 741 23 5 10 5.8 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
10742178 206051 0 None - 1 Human 6.0 pKi = 6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 449 5 0 3 5.2 O=C(c1ccc(Br)cc1)N(c1cccnc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL85511 206051 0 None - 1 Human 6.0 pKi = 6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 449 5 0 3 5.2 O=C(c1ccc(Br)cc1)N(c1cccnc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
44274441 99065 0 None -1 5 Human 5.0 pKi = 5 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL280684 99065 0 None -1 5 Human 5.0 pKi = 5 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
155552923 176283 0 None -213 5 Human 5.0 pKi = 5 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4544820 176283 0 None -213 5 Human 5.0 pKi = 5 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595245 176283 0 None -213 5 Human 5.0 pKi = 5 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
45786849 157781 34 None -1 3 Human 5.0 pKi = 5 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 3 1 3 1.4 c1cncc(COC2CCCNC2)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4083241 157781 34 None -1 3 Human 5.0 pKi = 5 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 3 1 3 1.4 c1cncc(COC2CCCNC2)c1 10.1021/acs.jmedchem.7b01113
56593934 65665 0 None -2630 8 Human 5.0 pKi = 5 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
CHEMBL1834350 65665 0 None -2630 8 Human 5.0 pKi = 5 Binding
Inhibition of human muscarinic M3 receptorInhibition of human muscarinic M3 receptor
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
1212 1649 50 None -407 66 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1649 50 None -407 66 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1649 50 None -407 66 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1649 50 None -407 66 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1649 50 None -407 66 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
16125444 168403 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 397 4 1 2 4.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(c2ccccc2)CC1 10.1021/jm061159a
CHEMBL434929 168403 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 397 4 1 2 4.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(c2ccccc2)CC1 10.1021/jm061159a
9998202 69137 0 None 2 2 Rat 7.0 pKi = 7.0 Binding
Ki value for rat Muscarinic acetylcholine receptor M3Ki value for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
CHEMBL192485 69137 0 None 2 2 Rat 7.0 pKi = 7.0 Binding
Ki value for rat Muscarinic acetylcholine receptor M3Ki value for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
155562295 175126 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 396 6 0 5 3.9 COc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4570052 175126 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 396 6 0 5 3.9 COc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1OC 10.1016/j.bmcl.2018.12.022
11015312 5242 0 None -15 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 5 1 5 4.9 CCCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL106505 5242 0 None -15 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 5 1 5 4.9 CCCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
324 1912 15 None -17 9 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
6436265 1912 15 None -17 9 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
CHEMBL277642 1912 15 None -17 9 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
145960827 161356 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@@H](CO[C@@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
CHEMBL4126290 161356 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@@H](CO[C@@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
2551 791 23 None -54 11 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
11024241 120275 0 None -1 5 Human 6.0 pKi = 6.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 338 6 0 3 4.9 CSc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
CHEMBL352723 120275 0 None -1 5 Human 6.0 pKi = 6.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 338 6 0 3 4.9 CSc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
164618698 188509 0 None -11220 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 23 10 13 -0.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4862098 188509 0 None -11220 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 23 10 13 -0.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028512 188509 0 None -11220 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 23 10 13 -0.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
46227485 14091 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198034 14091 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL593620 14091 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
16125565 84731 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 401 5 2 3 3.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2c[nH]cn2)CC1 10.1021/jm061159a
CHEMBL223022 84731 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 401 5 2 3 3.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2c[nH]cn2)CC1 10.1021/jm061159a
73350931 92505 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 279 3 0 2 2.4 CN(Cc1ccccc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432040 92505 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 279 3 0 2 2.4 CN(Cc1ccccc1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
109035013 180451 1 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 314 4 1 2 4.1 O=C(CCN1CCCc2ccccc21)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2020.127632
CHEMBL4752973 180451 1 None -3 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 314 4 1 2 4.1 O=C(CCN1CCCc2ccccc21)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2020.127632
15050952 203473 0 None -1 3 Rat 5.0 pKi = 5.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 507 9 3 7 1.0 CC(=O)NCCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL66177 203473 0 None -1 3 Rat 5.0 pKi = 5.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 507 9 3 7 1.0 CC(=O)NCCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
73350398 89769 0 None 10 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 363 8 0 4 5.0 CCN(CC)CCOC(=O)c1ccccc1Sc1ccc(Cl)cc1 10.1016/j.bmc.2013.01.072
CHEMBL2377262 89769 0 None 10 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 363 8 0 4 5.0 CCN(CC)CCOC(=O)c1ccccc1Sc1ccc(Cl)cc1 10.1016/j.bmc.2013.01.072
155566290 176556 0 None -1318 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4582879 176556 0 None -1318 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597498 176556 0 None -1318 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 916 24 9 11 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
11766733 155730 0 None -549 5 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1121 29 4 10 12.0 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
CHEMBL1202003 155730 0 None -549 5 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1121 29 4 10 12.0 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
CHEMBL405739 155730 0 None -549 5 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1121 29 4 10 12.0 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
49783415 17646 0 None -1479 13 Human 6.0 pKi = 6.0 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258452 17646 0 None -1479 13 Human 6.0 pKi = 6.0 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
154734599 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
327 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
4108 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
CHEMBL27673 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00075a032
156013536 178287 0 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4639297 178287 0 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651058 178287 0 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
154734599 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
327 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
4108 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
CHEMBL27673 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/0960-894X(95)00113-8
154734599 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00046a021
327 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00046a021
4108 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00046a021
CHEMBL27673 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm00046a021
44299599 167781 0 None -9 4 Human 5.0 pKi = 5.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](C#C[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL430587 167781 0 None -9 4 Human 5.0 pKi = 5.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](C#C[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
54816802 181248 2 None -26 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 2 0 2 2.5 O=C(CN1CCCc2ccccc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4762056 181248 2 None -26 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 2 0 2 2.5 O=C(CN1CCCc2ccccc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
46227413 14108 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 C[C@@H]1OC[C@@H](C[N+](C)(C)C)O[C@H]1C 10.1016/j.bmc.2009.10.027
CHEMBL1198087 14108 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 C[C@@H]1OC[C@@H](C[N+](C)(C)C)O[C@H]1C 10.1016/j.bmc.2009.10.027
CHEMBL595265 14108 0 None 1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 C[C@@H]1OC[C@@H](C[N+](C)(C)C)O[C@H]1C 10.1016/j.bmc.2009.10.027
44309153 203491 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 352 4 2 3 2.5 NCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL66322 203491 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 352 4 2 3 2.5 NCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
9905731 168484 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 334 6 1 5 2.2 CN(C)C1(CNCCC2CCOCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL435353 168484 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 334 6 1 5 2.2 CN(C)C1(CNCCC2CCOCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
156014558 177200 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 344 4 2 3 4.6 O=C(Nc1ccccc1-c1ccc(Cl)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4635566 177200 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 344 4 2 3 4.6 O=C(Nc1ccccc1-c1ccc(Cl)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
10716120 38253 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 402 7 2 3 3.9 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CC[C@@H](F)C2)CC1 10.1021/jm0003135
CHEMBL146249 38253 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 402 7 2 3 3.9 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CC[C@@H](F)C2)CC1 10.1021/jm0003135
10573458 119236 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 407 6 2 4 3.5 Cc1cccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)n1 10.1021/jm0003135
CHEMBL343659 119236 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 407 6 2 4 3.5 Cc1cccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)n1 10.1021/jm0003135
44337760 9233 0 None -2 2 Rat 8.0 pKi = 8.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 335 4 0 3 3.8 CN1CC2CC1C[C@H](OC(=O)C(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL110808 9233 0 None -2 2 Rat 8.0 pKi = 8.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 335 4 0 3 3.8 CN1CC2CC1C[C@H](OC(=O)C(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
73353378 89773 0 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 331 4 1 4 2.4 CN1CCC(OC(=O)C(CO)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2013.01.072
CHEMBL2377268 89773 0 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 331 4 1 4 2.4 CN1CCC(OC(=O)C(CO)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2013.01.072
137628800 160970 0 None -1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 248 4 0 1 2.8 C[N+](C)(C)CCc1cccc(OC(F)(F)F)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4089027 160970 0 None -1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 248 4 0 1 2.8 C[N+](C)(C)CCc1cccc(OC(F)(F)F)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116151 160970 0 None -1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 248 4 0 1 2.8 C[N+](C)(C)CCc1cccc(OC(F)(F)F)c1 10.1021/acs.jmedchem.7b01113
3055 1421 44 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
313 1421 44 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
7163 1421 44 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
CHEMBL936 1421 44 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
DB01231 1421 44 None -1 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1016/j.bmcl.2008.03.061
44337638 110539 0 None -1 2 Rat 5.0 pKi = 5.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
CHEMBL325322 110539 0 None -1 2 Rat 5.0 pKi = 5.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
16125508 84303 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 412 5 1 3 4.0 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccnc2)CC1 10.1021/jm061159a
CHEMBL221660 84303 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 412 5 1 3 4.0 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccnc2)CC1 10.1021/jm061159a
16125224 136725 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 471 7 1 4 4.6 COc1ccc(C2(c3ccc(OC)cc3)CN(C3CCN(Cc4ccccc4)CC3)C(=O)N2)cc1 10.1021/jm061159a
CHEMBL374099 136725 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 471 7 1 4 4.6 COc1ccc(C2(c3ccc(OC)cc3)CN(C3CCN(Cc4ccccc4)CC3)C(=O)N2)cc1 10.1021/jm061159a
10771937 21661 0 None -204 5 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 871 27 4 8 9.4 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
CHEMBL1202004 21661 0 None -204 5 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 871 27 4 8 9.4 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
CHEMBL131846 21661 0 None -204 5 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 871 27 4 8 9.4 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1021/jm981038d
44318851 104699 0 None -60 4 Human 4.9 pKi = 4.9 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 183 2 1 3 1.2 CCC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
CHEMBL310558 104699 0 None -60 4 Human 4.9 pKi = 4.9 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 183 2 1 3 1.2 CCC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
164613559 188462 0 None -3630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 874 21 9 12 0.2 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4856659 188462 0 None -3630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 874 21 9 12 0.2 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028196 188462 0 None -3630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 874 21 9 12 0.2 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
155557119 176487 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4555411 176487 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596899 176487 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
162353379 180938 0 None -6 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 3 0 2 2.1 O=C(CCN1CCCc2ccccc21)N1CCC1 10.1016/j.bmcl.2020.127632
CHEMBL4758449 180938 0 None -6 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 3 0 2 2.1 O=C(CCN1CCCc2ccccc21)N1CCC1 10.1016/j.bmcl.2020.127632
3675988 176811 66 None 1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc(C2CCCN2)c1 10.1021/jm800145d
CHEMBL461087 176811 66 None 1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc(C2CCCN2)c1 10.1021/jm800145d
155516095 170032 0 None -2 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 366 5 0 4 3.9 COc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4442996 170032 0 None -2 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 366 5 0 4 3.9 COc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1 10.1016/j.bmcl.2018.12.022
542182 102134 1 None -1 3 Rat 4.9 pKi = 4.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 465 8 3 7 0.8 NCCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL302604 102134 1 None -1 3 Rat 4.9 pKi = 4.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 465 8 3 7 0.8 NCCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
16125505 84749 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 6 1 2 4.7 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CCc2ccccc2)CC1 10.1021/jm061159a
CHEMBL223186 84749 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 6 1 2 4.7 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CCc2ccccc2)CC1 10.1021/jm061159a
11012712 57799 2 None -1 5 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 3 4.2 COc1ccc2c(c1)CC(CCN(C)C)=C2C(C)c1ccccn1 10.1021/jm020895l
CHEMBL167027 57799 2 None -1 5 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 3 4.2 COc1ccc2c(c1)CC(CCN(C)C)=C2C(C)c1ccccn1 10.1021/jm020895l
11000399 59065 0 None -2 5 Human 4.9 pKi = 4.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2ccncc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL169680 59065 0 None -2 5 Human 4.9 pKi = 4.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2ccncc2)c2ccccc2C1 10.1021/jm020895l
118719925 115753 0 None -158 8 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 330 7 1 3 2.8 O=C1CCc2ccccc2N1CCCN1CCC(CCCO)CC1 10.1021/jm501173q
CHEMBL3354072 115753 0 None -158 8 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 330 7 1 3 2.8 O=C1CCc2ccccc2N1CCCN1CCC(CCCO)CC1 10.1021/jm501173q
44400185 69297 0 None 1 2 Rat 6.9 pKi = 6.9 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 321 5 1 2 4.6 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@@]3(C)C2)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
CHEMBL192885 69297 0 None 1 2 Rat 6.9 pKi = 6.9 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 321 5 1 2 4.6 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@@]3(C)C2)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
59291324 112751 0 None -1 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.5 O=C(Nc1scnc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298593 112751 0 None -1 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.5 O=C(Nc1scnc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305622 112751 0 None -1 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 329 3 1 5 3.5 O=C(Nc1scnc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL5267836 193514 0 None -6 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1038 20 1 13 9.8 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(OC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
10835518 40297 0 None 16 3 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 412 6 2 3 4.6 O=C(NC1CCN(CC2CCCCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL148129 40297 0 None 16 3 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 412 6 2 3 4.6 O=C(NC1CCN(CC2CCCCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
44443735 94354 0 None 52 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 448 7 2 5 3.1 O=C(N[C@H]1[C@@H]2CN(CCc3ccc4c(c3)OCO4)C[C@@H]21)[C@](O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL250834 94354 0 None 52 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 448 7 2 5 3.1 O=C(N[C@H]1[C@@H]2CN(CCc3ccc4c(c3)OCO4)C[C@@H]21)[C@](O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
44443733 154760 0 None 45 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 382 7 2 3 3.5 CC(C)=CCCN1C[C@H]2[C@H](NC(=O)[C@](O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
CHEMBL400167 154760 0 None 45 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 382 7 2 3 3.5 CC(C)=CCCN1C[C@H]2[C@H](NC(=O)[C@](O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
44337747 109646 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 425 6 0 3 5.6 CC(C(=O)O[C@H]1CC2CC(C1)N(Cc1ccccc1)C2)(c1ccccc1)c1ccccc1 10.1021/jm00115a003
CHEMBL322582 109646 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 425 6 0 3 5.6 CC(C(=O)O[C@H]1CC2CC(C1)N(Cc1ccccc1)C2)(c1ccccc1)c1ccccc1 10.1021/jm00115a003
CHEMBL5076535 214422 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCCN(C)C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44308831 204372 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 380 6 2 3 3.2 CNCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL71933 204372 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 380 6 2 3 3.2 CNCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
15050955 102571 0 None -1 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 538 7 1 7 3.0 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCCN3C(=O)c4ccccc4C3=O)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL304112 102571 0 None -1 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 538 7 1 7 3.0 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCCN3C(=O)c4ccccc4C3=O)CC2)c2ccccc21 10.1021/jm00111a032
24936155 94593 0 None -199 7 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 508 4 2 3 5.1 CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 10.1016/j.bmcl.2007.10.109
CHEMBL252258 94593 0 None -199 7 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 508 4 2 3 5.1 CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 10.1016/j.bmcl.2007.10.109
137630127 161025 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 210 4 1 2 1.4 COc1cccc(C(O)C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4084607 161025 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 210 4 1 2 1.4 COc1cccc(C(O)C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116537 161025 0 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 210 4 1 2 1.4 COc1cccc(C(O)C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
137630848 161092 0 None -1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 213 3 0 3 1.5 C[N+]1(C)CCC(OCc2nccs2)C1 10.1021/acs.jmedchem.7b01113
CHEMBL4061390 161092 0 None -1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 213 3 0 3 1.5 C[N+]1(C)CCC(OCc2nccs2)C1 10.1021/acs.jmedchem.7b01113
CHEMBL4117131 161092 0 None -1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 213 3 0 3 1.5 C[N+]1(C)CCC(OCc2nccs2)C1 10.1021/acs.jmedchem.7b01113
71452790 79621 0 None 1 2 Rat 4.9 pKi = 4.9 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 169 1 0 3 0.6 CC(=O)O[C@H]1CC2CC1CN2C 10.1021/jm00090a006
CHEMBL2115122 79621 0 None 1 2 Rat 4.9 pKi = 4.9 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 169 1 0 3 0.6 CC(=O)O[C@H]1CC2CC1CN2C 10.1021/jm00090a006
164619973 188517 0 None -3630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 23 9 12 1.0 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4862996 188517 0 None -3630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 23 9 12 1.0 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028571 188517 0 None -3630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 902 23 9 12 1.0 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
10236758 115746 5 None -1230 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 115746 5 None -1230 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
109018479 181794 1 None -9 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 284 5 1 3 2.7 O=C(CCN1CCCc2ccccc21)NCc1ccco1 10.1016/j.bmcl.2020.127632
CHEMBL4778178 181794 1 None -9 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 284 5 1 3 2.7 O=C(CCN1CCCc2ccccc21)NCc1ccco1 10.1016/j.bmcl.2020.127632
7141656 176813 7 None -3 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc([C@H]2CCCN2)o1 10.1021/jm800145d
CHEMBL461089 176813 7 None -3 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc([C@H]2CCCN2)o1 10.1021/jm800145d
44311760 204476 0 None -316 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 510 8 0 5 5.0 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCN(C(=O)CCC)CC2)CC1 10.1016/s0960-894x(00)00457-1
CHEMBL72551 204476 0 None -316 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 510 8 0 5 5.0 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCN(C(=O)CCC)CC2)CC1 10.1016/s0960-894x(00)00457-1
71463063 83772 0 None -1 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205825 83772 0 None -1 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
44448419 12304 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 580 16 2 2 7.0 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CCC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185266 12304 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 580 16 2 2 7.0 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CCC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL403592 12304 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 580 16 2 2 7.0 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CCC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
10226457 12943 0 None -31 5 Human 6.9 pKi = 6.9 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 423 15 0 7 5.1 CC(=O)OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL1189471 12943 0 None -31 5 Human 6.9 pKi = 6.9 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 423 15 0 7 5.1 CC(=O)OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL538793 12943 0 None -31 5 Human 6.9 pKi = 6.9 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 423 15 0 7 5.1 CC(=O)OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
3013845 188725 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 729 21 5 11 5.1 CCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL505197 188725 1 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 729 21 5 11 5.1 CCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
155557119 176487 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4555411 176487 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4596899 176487 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 868 17 7 8 5.1 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
155548586 176573 0 None -234 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 562 12 6 6 2.5 N=C(N)NCCC[C@H](N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4537517 176573 0 None -234 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 562 12 6 6 2.5 N=C(N)NCCC[C@H](N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597611 176573 0 None -234 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 562 12 6 6 2.5 N=C(N)NCCC[C@H](N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
44409977 76025 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 6 2 5 3.9 Cc1c(NCc2cccs2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
CHEMBL205737 76025 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 6 2 5 3.9 Cc1c(NCc2cccs2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
44409961 139216 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 5 1 4 3.7 Cc1c(NC2CC2)nc(CC2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL378904 139216 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 5 1 4 3.7 Cc1c(NC2CC2)nc(CC2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
2551 791 23 None -54 11 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
162677513 183720 0 None -39 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 983 17 3 11 6.2 CN(C)c1ccc2c(-c3ccc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
CHEMBL4789147 183720 0 None -39 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 983 17 3 11 6.2 CN(C)c1ccc2c(-c3ccc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
CHEMBL4803695 183720 0 None -39 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 983 17 3 11 6.2 CN(C)c1ccc2c(-c3ccc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
155540315 172889 0 None -3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 398 7 0 5 4.0 COc1ccc(CCN(C(=O)OC2CCN(C)CC2)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4516350 172889 0 None -3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 398 7 0 5 4.0 COc1ccc(CCN(C(=O)OC2CCN(C)CC2)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL1200633 208577 3 None -4 8 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL None None None CC[C@H](C)[C@H]1O[C@]2(CC[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(CC[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O nan
162353393 179415 0 None -6 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 312 5 1 2 3.3 O=C(CCN1CCCc2ccccc21)NCc1cccc(F)c1 10.1016/j.bmcl.2020.127632
CHEMBL4740422 179415 0 None -6 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 312 5 1 2 3.3 O=C(CCN1CCCc2ccccc21)NCc1cccc(F)c1 10.1016/j.bmcl.2020.127632
44406520 135233 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 CO[C@]1(C#C[C@](O)(c2ccccc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL372566 135233 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 348 3 1 4 2.4 CO[C@]1(C#C[C@](O)(c2ccccc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
3652 4066 79 None -3 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57 4066 79 None -3 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809 4066 79 None -3 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
CHEMBL21536 4066 79 None -3 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
DB15357 4066 79 None -3 18 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
44430473 143626 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 3 0 4 3.2 CC1CN(c2cc(N3CCCCCC3)nc(C3CC3)n2)C1 10.1016/j.bmcl.2007.03.047
CHEMBL389992 143626 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 3 0 4 3.2 CC1CN(c2cc(N3CCCCCC3)nc(C3CC3)n2)C1 10.1016/j.bmcl.2007.03.047
44409558 75898 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 272 4 1 4 3.2 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205105 75898 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 272 4 1 4 3.2 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCC1 10.1016/j.bmcl.2006.01.006
10836338 39303 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 429 6 2 4 3.5 O=C(NC1CCN(Cc2ccccn2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL147105 39303 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 429 6 2 4 3.5 O=C(NC1CCN(Cc2ccccn2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
155525097 170926 0 None -165 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 712 13 1 10 5.5 CN1CC=C(c2nsnc2OCCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4455570 170926 0 None -165 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 712 13 1 10 5.5 CN1CC=C(c2nsnc2OCCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)CC1 10.1021/acs.jmedchem.8b01967
154059 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
2457 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
7483 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
CHEMBL1734 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
DB01591 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 10.1016/j.ejmech.2017.06.004
16125223 168875 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 397 5 1 2 4.2 O=C1NC(c2ccccc2)(c2ccccc2)CN1[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm061159a
CHEMBL438427 168875 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 397 5 1 2 4.2 O=C1NC(c2ccccc2)(c2ccccc2)CN1[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm061159a
16125509 169318 0 None 69 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 417 5 1 3 4.7 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccs2)CC1 10.1021/jm061159a
CHEMBL441873 169318 0 None 69 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 417 5 1 3 4.7 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccs2)CC1 10.1021/jm061159a
155523648 176569 0 None -91 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 909 18 6 9 5.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4454300 176569 0 None -91 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 909 18 6 9 5.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597576 176569 0 None -91 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 909 18 6 9 5.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
10225340 204311 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 441 6 0 5 4.8 COc1ccc(S(=O)(=O)c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL71531 204311 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 441 6 0 5 4.8 COc1ccc(S(=O)(=O)c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
16125566 141507 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 445 5 1 2 5.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccccc2Cl)CC1 10.1021/jm061159a
CHEMBL384670 141507 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 445 5 1 2 5.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccccc2Cl)CC1 10.1021/jm061159a
155551306 173937 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 396 6 0 3 4.8 Cc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
CHEMBL4541518 173937 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 396 6 0 3 4.8 Cc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
3013846 188215 2 None 1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 757 23 5 11 5.9 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL499519 188215 2 None 1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 757 23 5 11 5.9 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
11567493 201779 13 None -5 3 Rat 5.9 pKi = 5.9 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccccc1 10.1021/jm050099q
CHEMBL606902 201779 13 None -5 3 Rat 5.9 pKi = 5.9 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccccc1 10.1021/jm050099q
10105296 205899 0 None -4 4 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 231 2 1 3 2.1 O=C(OC1CC2CCCC1N2)c1ccccc1 10.1021/jm9904001
CHEMBL84113 205899 0 None -4 4 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 231 2 1 3 2.1 O=C(OC1CC2CCCC1N2)c1ccccc1 10.1021/jm9904001
10386 161144 16 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 180 3 1 1 1.6 C[N+](C)(C)CCc1cccc(O)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4092348 161144 16 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 180 3 1 1 1.6 C[N+](C)(C)CCc1cccc(O)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4117554 161144 16 None 1 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 180 3 1 1 1.6 C[N+](C)(C)CCc1cccc(O)c1 10.1021/acs.jmedchem.7b01113
73346336 92516 0 None -2 6 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 2 3.0 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432054 92516 0 None -2 6 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 325 5 0 2 3.0 CN(CCCc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
71449073 78553 0 None -3 4 Rat 5.9 pKi = 5.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 338 2 2 6 0.6 O=C1Nc2cccnc2N(C(=O)CN2CCNCC2)c2ncccc21 10.1021/jm00111a032
CHEMBL2112217 78553 0 None -3 4 Rat 5.9 pKi = 5.9 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 338 2 2 6 0.6 O=C1Nc2cccnc2N(C(=O)CN2CCNCC2)c2ncccc21 10.1021/jm00111a032
164610746 188443 0 None -3388 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4854886 188443 0 None -3388 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028038 188443 0 None -3388 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
156015051 178304 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4643329 178304 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651139 178304 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
156009660 178305 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4634475 178305 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4651150 178305 0 None -3 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 360 5 0 3 3.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc([S+]([O-])c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
155549890 173884 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CCCN(C)C2)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4540291 173884 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CCCN(C)C2)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
135423423 188982 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 813 27 5 11 7.5 CCCCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL508807 188982 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 813 27 5 11 7.5 CCCCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
156010212 178213 0 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COC(c2ccccc2)(c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4634066 178213 0 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COC(c2ccccc2)(c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650562 178213 0 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COC(c2ccccc2)(c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
137645938 157559 0 None -977 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 342 8 0 2 4.6 CCCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4080675 157559 0 None -977 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 342 8 0 2 4.6 CCCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
657347 5044 2 None -114 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.5 C[C@H]1OC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
CHEMBL105457 5044 2 None -114 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.5 C[C@H]1OC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
CHEMBL387632 5044 2 None -114 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.5 C[C@H]1OC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
107782 14436 18 None -1 5 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
67151996 14436 18 None -1 5 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
CHEMBL1201207 14436 18 None -1 5 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O nan
1224 1420 83 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1420 83 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1420 83 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1420 83 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1420 83 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1420 83 None -5 13 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3191 102831 97 None -6 25 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102831 97 None -6 25 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
10595006 11413 0 None -8 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
CHEMBL1180343 11413 0 None -8 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
CHEMBL123099 11413 0 None -8 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1 10.1021/jm301774u
10104 3540 12 None -4 6 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
6604866 3540 12 None -4 6 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
CHEMBL1493369 3540 12 None -4 6 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 10.1021/jm020895l
155525065 176530 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 590 11 4 6 2.9 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4456524 176530 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 590 11 4 6 2.9 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597243 176530 0 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 590 11 4 6 2.9 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
10874119 4875 0 None -19 5 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 454 4 1 5 5.3 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(C(=O)OCc5ccccc5)c34)OC21 10.1021/jm011116o
CHEMBL104574 4875 0 None -19 5 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 454 4 1 5 5.3 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(C(=O)OCc5ccccc5)c34)OC21 10.1021/jm011116o
2551 791 23 None -54 11 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
53324553 56825 0 None -1 10 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
CHEMBL1643900 56825 0 None -1 10 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmcl.2010.11.075
53324553 56825 0 None -1 10 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
CHEMBL1643900 56825 0 None -1 10 Human 5.9 pKi = 5.9 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 283 4 1 1 3.1 Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1 10.1016/j.bmc.2013.07.045
44400323 68640 0 None 2 2 Rat 7.9 pKi = 7.9 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 361 5 1 4 2.4 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2005.02.036
CHEMBL192065 68640 0 None 2 2 Rat 7.9 pKi = 7.9 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 361 5 1 4 2.4 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2005.02.036
44431386 149001 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 332 5 1 5 2.1 CN(C)C1(CNCC=C2CCOCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL394255 149001 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 332 5 1 5 2.1 CN(C)C1(CNCC=C2CCOCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
53321085 58486 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 366 7 1 3 5.6 CCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683913 58486 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 366 7 1 3 5.6 CCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL5271406 193657 0 None -3 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1159 27 3 10 12.8 CC1(C)C(/C=C/C=C/C=C2/N(CCCCS(=O)(=O)O)c3ccccc3C2(C)C)=[N+](CCCCCC(=O)NCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(F)c(Cl)c3)CC2)c2ccc(S(=O)(=O)[O-])cc21 10.1021/acs.jmedchem.2c01376
138710710 177021 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1ccc(Cl)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4632545 177021 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1ccc(Cl)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
11794901 119557 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 393 6 2 4 3.2 O=C(NC1CCN(Cc2ccccn2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL346194 119557 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 393 6 2 4 3.2 O=C(NC1CCN(Cc2ccccn2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
53372934 129274 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670826 129274 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
156015390 178218 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4648229 178218 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650585 178218 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
53319789 58514 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 667 16 5 6 7.1 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1C[N+]2(CCCCCCCCCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)CCC1CC2 10.1016/j.bmcl.2011.01.043
CHEMBL1683941 58514 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 667 16 5 6 7.1 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1C[N+]2(CCCCCCCCCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)CCC1CC2 10.1016/j.bmcl.2011.01.043
137629887 160986 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 218 4 0 1 3.1 C[N+](C)(C)CCCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
CHEMBL4065555 160986 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 218 4 0 1 3.1 C[N+](C)(C)CCCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116259 160986 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 218 4 0 1 3.1 C[N+](C)(C)CCCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
155535972 172098 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 356 5 0 3 4.1 CN1CCC(OC(=O)N(CCc2ccc(F)cc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.12.022
CHEMBL4472832 172098 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 356 5 0 3 4.1 CN1CCC(OC(=O)N(CCc2ccc(F)cc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.12.022
71720488 86924 0 None -2 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 337 3 0 5 2.7 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)c3ccccc3Cl)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323441 86924 0 None -2 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 337 3 0 5 2.7 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)c3ccccc3Cl)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
137628799 160969 0 None -14 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 212 4 0 1 2.1 COc1ccc(F)c(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4064668 160969 0 None -14 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 212 4 0 1 2.1 COc1ccc(F)c(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116150 160969 0 None -14 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 212 4 0 1 2.1 COc1ccc(F)c(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
1836 2574 59 None -42 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 2574 59 None -42 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 2574 59 None -42 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 2574 59 None -42 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 2574 59 None -42 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
44337638 110539 0 None -1 2 Rat 4.9 pKi = 4.9 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
CHEMBL325322 110539 0 None -1 2 Rat 4.9 pKi = 4.9 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
44274302 77038 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL20732 77038 0 None -1 5 Human 4.9 pKi = 4.9 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
137640511 157042 0 None -54 8 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 286 4 0 2 3.1 CC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4074104 157042 0 None -54 8 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 286 4 0 2 3.1 CC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
156014450 178227 0 None -794 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 518 9 2 6 3.4 NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4636083 178227 0 None -794 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 518 9 2 6 3.4 NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4650652 178227 0 None -794 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 518 9 2 6 3.4 NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
145961152 161567 0 None -8 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4129382 161567 0 None -8 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
44437259 11847 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 297 4 0 3 3.0 C[N+]1(CC#CCOc2cc(-c3ccccc3)on2)CCCC1 10.1016/j.bmc.2007.09.003
CHEMBL1182448 11847 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 297 4 0 3 3.0 C[N+]1(CC#CCOc2cc(-c3ccccc3)on2)CCCC1 10.1016/j.bmc.2007.09.003
CHEMBL239038 11847 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 297 4 0 3 3.0 C[N+]1(CC#CCOc2cc(-c3ccccc3)on2)CCCC1 10.1016/j.bmc.2007.09.003
156014820 178281 0 None -69 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4646116 178281 0 None -69 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4650998 178281 0 None -69 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02172
132947 3835 9 None -309 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/j.bmc.2008.06.025
361 3835 9 None -309 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/j.bmc.2008.06.025
CHEMBL265256 3835 9 None -309 9 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/j.bmc.2008.06.025
156014820 178281 0 None -69 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
CHEMBL4646116 178281 0 None -69 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
CHEMBL4650998 178281 0 None -69 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 780 14 1 6 7.8 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
132947 3835 9 None -999 9 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm981038d
361 3835 9 None -999 9 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm981038d
CHEMBL265256 3835 9 None -999 9 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm981038d
155521383 176402 0 None -131 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 604 13 6 6 2.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4450522 176402 0 None -131 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 604 13 6 6 2.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596184 176402 0 None -131 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 604 13 6 6 2.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
46878250 201836 0 None -1 2 Rat 4.8 pKi = 4.8 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@H]1CC2CC(C1)N([C@H](C)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL607175 201836 0 None -1 2 Rat 4.8 pKi = 4.8 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@H]1CC2CC(C1)N([C@H](C)c1ccccc1)C2 10.1021/jm00115a003
3158 56237 27 None -104 20 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 56237 27 None -104 20 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
10670961 40602 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 444 6 3 5 3.1 Nc1ccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)nc1 10.1021/jm0003135
CHEMBL148404 40602 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 444 6 3 5 3.1 Nc1ccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)nc1 10.1021/jm0003135
137630050 161016 0 None -42 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 1358 31 7 15 8.7 CCC(=O)NCc1cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)c1 10.1021/acs.jmedchem.6b01892
CHEMBL4089543 161016 0 None -42 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 1358 31 7 15 8.7 CCC(=O)NCc1cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)c1 10.1021/acs.jmedchem.6b01892
CHEMBL4097258 161016 0 None -42 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 1358 31 7 15 8.7 CCC(=O)NCc1cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)c1 10.1021/acs.jmedchem.6b01892
CHEMBL4116470 161016 0 None -42 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 1358 31 7 15 8.7 CCC(=O)NCc1cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)cc(C(=O)NCCNC(=O)CCc2cn(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)cn2)c1 10.1021/acs.jmedchem.6b01892
10171655 86977 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 3 0 4 3.3 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCC1 10.1016/j.bmcl.2007.03.047
CHEMBL232419 86977 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 3 0 4 3.3 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCC1 10.1016/j.bmcl.2007.03.047
10269809 159357 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 345 3 0 2 4.1 COC1(C#CC(C)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL410061 159357 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 345 3 0 2 4.1 COC1(C#CC(C)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
44319010 205803 0 None 15 2 Human 7.8 pKi = 7.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 348 5 0 2 4.5 O=C(C1CCC1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL83363 205803 0 None 15 2 Human 7.8 pKi = 7.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 348 5 0 2 4.5 O=C(C1CCC1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
46878242 201788 0 None -13 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1C[C@H](O)c2ccccc2[C@H]1c1ccccc1 10.1021/jm050099q
CHEMBL606962 201788 0 None -13 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1C[C@H](O)c2ccccc2[C@H]1c1ccccc1 10.1021/jm050099q
16086015 12269 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 1 4 4.6 NCC1CCN(C(=O)[C@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)CC(c2ccccc2)(c2ccccc2)c2ccccc2)CC1 10.1021/jm051205r
CHEMBL1184933 12269 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 1 4 4.6 NCC1CCN(C(=O)[C@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)CC(c2ccccc2)(c2ccccc2)c2ccccc2)CC1 10.1021/jm051205r
CHEMBL379055 12269 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 1 4 4.6 NCC1CCN(C(=O)[C@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)CC(c2ccccc2)(c2ccccc2)c2ccccc2)CC1 10.1021/jm051205r
CHEMBL306462 102938 0 None -1 5 Human 5.8 pKi = 5.8 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 211 2 1 4 1.1 CCO/C(O)=C1\CN2CCCC(C2)C1=O 10.1021/jm020572p
44328540 207759 0 None -4 3 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 245 3 1 3 2.3 COc1ccccc1C(O)C1=CN2CCC1CC2 10.1016/S0960-894X(01)80824-6
CHEMBL96042 207759 0 None -4 3 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 245 3 1 3 2.3 COc1ccccc1C(O)C1=CN2CCC1CC2 10.1016/S0960-894X(01)80824-6
10035281 100955 0 None -6 8 Human 4.8 pKi = 4.8 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
CHEMBL294273 100955 0 None -6 8 Human 4.8 pKi = 4.8 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
10035281 100955 0 None -6 8 Rat 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
CHEMBL294273 100955 0 None -6 8 Rat 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
10035281 100955 0 None -6 8 Human 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
CHEMBL294273 100955 0 None -6 8 Human 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 183 1 0 3 1.2 CC(=O)OC1CC2CCCC1N2C 10.1021/jm9705115
10160073 111162 0 None -151 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm301774u
CHEMBL326450 111162 0 None -151 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm301774u
155543944 176310 0 None -426 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 873 21 6 10 2.3 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4567026 176310 0 None -426 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 873 21 6 10 2.3 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595467 176310 0 None -426 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 873 21 6 10 2.3 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
10160073 111162 0 None -151 5 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL326450 111162 0 None -151 5 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 434 6 1 5 5.1 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
639794 98741 1 None -1 5 Human 4.8 pKi = 4.8 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL278129 98741 1 None -1 5 Human 4.8 pKi = 4.8 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 320 5 0 4 3.1 CN(C)CCOC(=O)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
19021478 192673 0 None -11 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to Muscarinic acetylcholine receptor M3 (unknown origin) assessed as inhibition constantBinding affinity to Muscarinic acetylcholine receptor M3 (unknown origin) assessed as inhibition constant
ChEMBL 356 4 1 3 4.5 CNC(=O)Oc1cccc2c1CCC1C2CCN1CCC1CCCCC1 10.1016/j.ejmech.2022.114606
CHEMBL5219452 192673 0 None -11 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to Muscarinic acetylcholine receptor M3 (unknown origin) assessed as inhibition constantBinding affinity to Muscarinic acetylcholine receptor M3 (unknown origin) assessed as inhibition constant
ChEMBL 356 4 1 3 4.5 CNC(=O)Oc1cccc2c1CCC1C2CCN1CCC1CCCCC1 10.1016/j.ejmech.2022.114606
16125437 84319 0 None 19 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 439 7 1 2 4.9 O=C1NC(Cc2ccccc2)(Cc2ccccc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL221713 84319 0 None 19 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 439 7 1 2 4.9 O=C1NC(Cc2ccccc2)(Cc2ccccc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
44420791 84675 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 376 3 1 1 3.7 C[N+]1(C)C2CCC1CC(N1CC(c3ccccc3)(c3ccccc3)NC1=O)C2 10.1021/jm061160+
CHEMBL222689 84675 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 376 3 1 1 3.7 C[N+]1(C)C2CCC1CC(N1CC(c3ccccc3)(c3ccccc3)NC1=O)C2 10.1021/jm061160+
155554568 176585 0 None -363 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 702 14 4 8 2.6 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4548432 176585 0 None -363 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 702 14 4 8 2.6 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597724 176585 0 None -363 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 702 14 4 8 2.6 CC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
156016041 178223 0 None -38 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1238 28 4 13 9.9 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCNC(=O)CCc3cn(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)cn3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4644612 178223 0 None -38 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1238 28 4 13 9.9 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCNC(=O)CCc3cn(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)cn3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650627 178223 0 None -38 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1238 28 4 13 9.9 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCNC(=O)CCc3cn(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)cn3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
44627956 14002 0 None -3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197362 14002 0 None -3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL568775 14002 0 None -3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
101676031 97299 0 None -32 4 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
16175987 97299 0 None -32 4 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL1201998 97299 0 None -32 4 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL269272 97299 0 None -32 4 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
122194376 123865 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 366 7 1 3 3.4 COc1ccc(CCC(=O)NCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
CHEMBL3627739 123865 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 366 7 1 3 3.4 COc1ccc(CCC(=O)NCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
10880435 59029 0 None -6 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL169494 59029 0 None -6 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
156015719 178234 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4646457 178234 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650699 178234 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
145961981 161507 0 None -7 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@]1(C(=O)O[C@@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4128497 161507 0 None -7 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@]1(C(=O)O[C@@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
11729182 5199 0 None -3 5 Human 4.8 pKi = 4.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 405 3 1 4 4.0 CCN(C)C(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL106259 5199 0 None -3 5 Human 4.8 pKi = 4.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 405 3 1 4 4.0 CCN(C)C(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
155521639 170670 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 424 8 0 5 4.4 COc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4451822 170670 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 424 8 0 5 4.4 COc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1OC 10.1016/j.bmcl.2018.12.022
2200 3109 46 None -7 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
328 3109 46 None -7 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
4848 3109 46 None -7 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
CHEMBL9967 3109 46 None -7 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
DB00670 3109 46 None -7 13 Human 6.8 pKi = 6.8 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm301774u
44430462 92277 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 302 3 1 5 2.2 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(O)C1 10.1016/j.bmcl.2007.03.047
CHEMBL242822 92277 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 302 3 1 5 2.2 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(O)C1 10.1016/j.bmcl.2007.03.047
44409654 75499 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 326 4 1 4 4.4 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC2(CCCC2)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL204353 75499 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 326 4 1 4 4.4 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC2(CCCC2)CC1 10.1016/j.bmcl.2006.01.006
129989 450 51 None -48 9 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00075a032
8584 450 51 None -48 9 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00075a032
CHEMBL43383 450 51 None -48 9 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00075a032
44430467 152065 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 304 3 0 4 3.2 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(F)C1 10.1016/j.bmcl.2007.03.047
CHEMBL396761 152065 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 304 3 0 4 3.2 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(F)C1 10.1016/j.bmcl.2007.03.047
44319008 205739 0 None 2 2 Human 6.8 pKi = 6.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 386 4 0 2 4.5 CC(=O)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL82850 205739 0 None 2 2 Human 6.8 pKi = 6.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 386 4 0 2 4.5 CC(=O)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
44318969 206057 0 None 3 2 Human 6.8 pKi = 6.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 384 6 0 2 5.0 O=C(c1ccccc1)N(Cc1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL85568 206057 0 None 3 2 Human 6.8 pKi = 6.8 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 384 6 0 2 5.0 O=C(c1ccccc1)N(Cc1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
10651844 115463 0 None -16 5 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 649 22 3 7 5.2 CN(CCCCCCCCN(C)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
CHEMBL335115 115463 0 None -16 5 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 649 22 3 7 5.2 CN(CCCCCCCCN(C)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
155554262 176531 0 None -47 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 797 15 6 7 5.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4582069 176531 0 None -47 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 797 15 6 7 5.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597244 176531 0 None -47 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 797 15 6 7 5.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
16094788 141890 0 None -125 5 Human 5.8 pKi = 5.8 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL386983 141890 0 None -125 5 Human 5.8 pKi = 5.8 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
6726 1269 51 None -6 13 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
7151 1269 51 None -6 13 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
749 1269 51 None -6 13 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL648 1269 51 None -6 13 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB01176 1269 51 None -6 13 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
44308913 203944 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 381 4 2 4 0.9 NCC(=O)N1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL69402 203944 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 381 4 2 4 0.9 NCC(=O)N1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
5282593 55228 26 None -1 5 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
CHEMBL1319362 55228 26 None -1 5 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
CHEMBL1618018 55228 26 None -1 5 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2 nan
10171655 86977 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 3 0 4 3.3 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCC1 10.1016/j.bmcl.2007.03.047
CHEMBL232419 86977 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 3 0 4 3.3 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCC1 10.1016/j.bmcl.2007.03.047
44409759 76005 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205686 76005 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCCC1 10.1016/j.bmcl.2006.01.006
10236397 77283 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 4 3.5 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(C)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL208280 77283 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 4 3.5 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(C)CC1 10.1016/j.bmcl.2006.01.006
11796409 38361 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 420 7 2 3 4.2 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CCC(F)(F)C2)CC1 10.1021/jm0003135
CHEMBL146351 38361 0 None 3 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 420 7 2 3 4.2 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CCC(F)(F)C2)CC1 10.1021/jm0003135
155521894 176401 0 None -204 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4451383 176401 0 None -204 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596183 176401 0 None -204 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
16125568 97301 0 None 17 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 445 5 1 2 5.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1021/jm061159a
CHEMBL269280 97301 0 None 17 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 445 5 1 2 5.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1021/jm061159a
16124710 85156 0 None 54 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 412 5 0 3 5.0 O=C1OC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL225387 85156 0 None 54 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 412 5 0 3 5.0 O=C1OC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
156015648 178291 0 None -87 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1021 18 5 12 5.5 NCc1cc(C(=O)NCCN2CCC(N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CC2)cc(C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)c1 10.1021/acs.jmedchem.9b02172
CHEMBL4641328 178291 0 None -87 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1021 18 5 12 5.5 NCc1cc(C(=O)NCCN2CCC(N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CC2)cc(C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)c1 10.1021/acs.jmedchem.9b02172
CHEMBL4651078 178291 0 None -87 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1021 18 5 12 5.5 NCc1cc(C(=O)NCCN2CCC(N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CC2)cc(C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)c1 10.1021/acs.jmedchem.9b02172
15157140 99846 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 359 10 0 3 5.2 CCN(CC)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL285898 99846 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 359 10 0 3 5.2 CCN(CC)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
11718570 72173 0 None -8 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 376 3 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1Cc1ccccc1 10.1021/jm050099q
CHEMBL198065 72173 0 None -8 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 376 3 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1Cc1ccccc1 10.1021/jm050099q
11532924 138357 0 None -47 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to muscarinic M3RBinding affinity to muscarinic M3R
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL377241 138357 0 None -47 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to muscarinic M3RBinding affinity to muscarinic M3R
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
137628855 160946 0 None -5 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 1 1 1 2.0 C[N+](C)(C)C1CCc2cccc(O)c2C1 10.1021/acs.jmedchem.7b01113
CHEMBL4103087 160946 0 None -5 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 1 1 1 2.0 C[N+](C)(C)C1CCc2cccc(O)c2C1 10.1021/acs.jmedchem.7b01113
CHEMBL4115966 160946 0 None -5 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 1 1 1 2.0 C[N+](C)(C)C1CCc2cccc(O)c2C1 10.1021/acs.jmedchem.7b01113
71452387 83774 0 None -1 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2012.08.046
CHEMBL2205829 83774 0 None -1 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2012.08.046
71452387 83774 0 None -1 7 Human 5.8 pKi = 5.8 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL2205829 83774 0 None -1 7 Human 5.8 pKi = 5.8 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 309 2 1 4 1.7 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccc2c(c1)OCO2 10.1016/j.bmc.2013.07.045
1547484 937 74 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
654 937 74 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
9072 937 74 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
CHEMBL43064 937 74 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
DB00568 937 74 None -5 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 nan
44593626 187829 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496306 187829 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL539121 187829 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
10360219 101983 0 None -16 4 Human 5.8 pKi = 5.8 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](/C=C/[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL301670 101983 0 None -16 4 Human 5.8 pKi = 5.8 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](/C=C/[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
155559741 176263 0 None -891 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4562770 176263 0 None -891 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595125 176263 0 None -891 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 739 17 6 8 4.0 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
145961126 161529 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@@]1(C(=O)O[C@@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4128764 161529 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@@]1(C(=O)O[C@@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
46227483 14093 0 None 1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198039 14093 0 None 1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL593685 14093 0 None 1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
16125506 84750 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 439 7 1 2 5.1 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CCCc2ccccc2)CC1 10.1021/jm061159a
CHEMBL223187 84750 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 439 7 1 2 5.1 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CCCc2ccccc2)CC1 10.1021/jm061159a
44275807 98942 0 None -1513 10 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human muscarinic M3 receptorBinding affinity towards human muscarinic M3 receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
CHEMBL27979 98942 0 None -1513 10 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human muscarinic M3 receptorBinding affinity towards human muscarinic M3 receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
44627856 197466 0 None -1 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569953 197466 0 None -1 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
9998508 80081 0 None -4 5 Human 5.8 pKi = 5.8 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21321 80081 0 None -4 5 Human 5.8 pKi = 5.8 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
156015968 178221 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4648657 178221 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650620 178221 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
156015809 178294 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(Sc3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4645019 178294 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(Sc3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651096 178294 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(Sc3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
145962050 161608 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4130037 161608 0 None -8 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
44309089 102983 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 352 5 3 3 2.4 O=C(NCC1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL306903 102983 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 352 5 3 3 2.4 O=C(NCC1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
44309208 165625 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 3 2 3 2.1 O=C(N1CCCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL424416 165625 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 3 2 3 2.1 O=C(N1CCCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
135398737 955 93 None -10 92 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 955 93 None -10 92 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 955 93 None -10 92 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 955 93 None -10 92 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 955 93 None -10 92 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
53321084 58485 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 352 6 1 3 5.2 CCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683912 58485 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 352 6 1 3 5.2 CCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
140844410 176368 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 10 1 3 5.5 O=C(OC1C[N+]2(CCCCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4436947 176368 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 10 1 3 5.5 O=C(OC1C[N+]2(CCCCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4595946 176368 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 484 10 1 3 5.5 O=C(OC1C[N+]2(CCCCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
10647553 39688 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 458 7 3 4 3.6 O=C(NC1CCN(Cc2cccc(CO)c2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL147554 39688 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 458 7 3 4 3.6 O=C(NC1CCN(Cc2cccc(CO)c2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
10739662 42246 0 None 11 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 398 6 2 3 4.2 O=C(NC1CCN(CC2CCCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL149769 42246 0 None 11 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 398 6 2 3 4.2 O=C(NC1CCN(CC2CCCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
44568347 191627 0 None -8 15 Human 6.8 pKi = 6.8 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL519609 191627 0 None -8 15 Human 6.8 pKi = 6.8 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 356 6 0 4 5.2 CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
16086035 11793 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 2 4 4.8 NC1CCCC(NC(=O)[C@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)CC(c2ccccc2)(c2ccccc2)c2ccccc2)C1 10.1021/jm051205r
CHEMBL1182110 11793 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 2 4 4.8 NC1CCCC(NC(=O)[C@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)CC(c2ccccc2)(c2ccccc2)c2ccccc2)C1 10.1021/jm051205r
CHEMBL212530 11793 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 2 4 4.8 NC1CCCC(NC(=O)[C@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)CC(c2ccccc2)(c2ccccc2)c2ccccc2)C1 10.1021/jm051205r
44328356 111449 0 None - 1 Human 4.8 pKi = 4.8 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 305 1 1 3 3.6 OC1(C2=CN3CCC2CC3)c2ccccc2Oc2ccccc21 10.1016/S0960-894X(01)80824-6
CHEMBL327664 111449 0 None - 1 Human 4.8 pKi = 4.8 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 305 1 1 3 3.6 OC1(C2=CN3CCC2CC3)c2ccccc2Oc2ccccc21 10.1016/S0960-894X(01)80824-6
71459604 83764 0 None -3 14 Human 5.8 pKi = 5.8 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 83764 0 None -3 14 Human 5.8 pKi = 5.8 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
71455894 83773 0 None -1 12 Human 5.8 pKi = 5.8 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
CHEMBL2205827 83773 0 None -1 12 Human 5.8 pKi = 5.8 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmcl.2012.08.046
71455894 83773 0 None -1 12 Human 5.8 pKi = 5.8 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmc.2013.07.045
CHEMBL2205827 83773 0 None -1 12 Human 5.8 pKi = 5.8 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 325 4 1 4 2.0 COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC 10.1016/j.bmc.2013.07.045
2200 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
328 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
4848 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
CHEMBL9967 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
DB00670 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00075a032
2200 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
328 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
4848 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
CHEMBL9967 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
DB00670 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00403-G
164627445 188583 0 None -812 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 831 21 8 11 1.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4876453 188583 0 None -812 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 831 21 8 11 1.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028997 188583 0 None -812 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 831 21 8 11 1.5 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
2200 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
328 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
4848 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
CHEMBL9967 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
DB00670 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/0960-894X(95)00113-8
2200 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00046a021
328 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00046a021
4848 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00046a021
CHEMBL9967 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00046a021
DB00670 3109 46 None -11 13 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00046a021
14939891 169340 0 None -239 4 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL442014 169340 0 None -239 4 Rat 6.8 pKi = 6.8 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
10043954 82249 0 None -5 5 Human 5.8 pKi = 5.8 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21716 82249 0 None -5 5 Human 5.8 pKi = 5.8 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
46682613 181132 1 None -31 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 4 1 2 3.3 O=C(CCN1CCCc2ccccc21)NC1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4760823 181132 1 None -31 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 4 1 2 3.3 O=C(CCN1CCCc2ccccc21)NC1CCCCC1 10.1016/j.bmcl.2020.127632
44448417 11877 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 550 16 2 4 6.7 CN(CCCN(C)CCCC(O)(c1ccccc1)c1ccccc1)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1182629 11877 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 550 16 2 4 6.7 CN(CCCN(C)CCCC(O)(c1ccccc1)c1ccccc1)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL256923 11877 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 550 16 2 4 6.7 CN(CCCN(C)CCCC(O)(c1ccccc1)c1ccccc1)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
11759379 120751 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 332 5 0 2 5.1 CC(C1=C(CCN2CCCCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL355392 120751 0 None -2 5 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 332 5 0 2 5.1 CC(C1=C(CCN2CCCCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
57326140 77150 0 None -2 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL2042400 77150 0 None -2 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL2078962 77150 0 None -2 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
14925759 158014 6 None -6165 13 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 158014 6 None -6165 13 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
24894635 169783 0 None -1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@@H]1c1ccco1 10.1021/jm800145d
CHEMBL443939 169783 0 None -1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@@H]1c1ccco1 10.1021/jm800145d
CHEMBL527880 169783 0 None -1 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@@H]1c1ccco1 10.1021/jm800145d
15157141 92772 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 373 11 0 3 5.6 CCN(CC)CCCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL24369 92772 0 None -1 4 Human 6.8 pKi = 6.8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 373 11 0 3 5.6 CCN(CC)CCCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
2247 504 81 None -19 42 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 504 81 None -19 42 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 504 81 None -19 42 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 504 81 None -19 42 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 504 81 None -19 42 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
73346332 92506 0 None -1 4 Human 5.8 pKi = 5.8 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 297 3 0 2 2.6 CN(Cc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
CHEMBL2432041 92506 0 None -1 4 Human 5.8 pKi = 5.8 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 297 3 0 2 2.6 CN(Cc1cccc(F)c1)[C@H]1C2C3CC4C2C(=O)C2C4C3C21 10.1016/j.bmc.2013.07.045
11501540 133578 0 None -3 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1c1cccs1 10.1021/jm050099q
CHEMBL371293 133578 0 None -3 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1c1cccs1 10.1021/jm050099q
44431369 87954 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 340 6 1 4 2.9 Cc1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 10.1016/j.bmcl.2006.11.058
CHEMBL234253 87954 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 340 6 1 4 2.9 Cc1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 10.1016/j.bmcl.2006.11.058
90666104 109308 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3O)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219034 109308 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3O)CC2)ccc1O 10.1039/C1MD00140J
44610361 123962 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 698 14 5 9 4.9 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc(C(O)(c6ccccc6)c6ccccc6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629357 123962 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 698 14 5 9 4.9 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc(C(O)(c6ccccc6)c6ccccc6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
10622718 38372 0 None 7 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 434 6 2 3 4.5 O=C(NC1CCN(CC2CCCCC2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL146359 38372 0 None 7 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 434 6 2 3 4.5 O=C(NC1CCN(CC2CCCCC2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
44364174 121959 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 400 7 3 4 3.0 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CC[C@H](O)C2)CC1 10.1021/jm0003135
CHEMBL359220 121959 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 400 7 3 4 3.0 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CC[C@H](O)C2)CC1 10.1021/jm0003135
44593619 187436 0 None -2 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493980 187436 0 None -2 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
16124708 137311 0 None 28 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 0 2 5.0 CN1C(=O)N(C2CCN(Cc3ccccc3)CC2)CC1(c1ccccc1)c1ccccc1 10.1021/jm061159a
CHEMBL375277 137311 0 None 28 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 0 2 5.0 CN1C(=O)N(C2CCN(Cc3ccccc3)CC2)CC1(c1ccccc1)c1ccccc1 10.1021/jm061159a
44304818 203283 0 None -67 7 Rat 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64788 203283 0 None -67 7 Rat 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
44304818 203283 0 None -67 7 Human 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64788 203283 0 None -67 7 Human 4.8 pKi = 4.8 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.7 COC(=O)C1CC2CCCC1N2 10.1021/jm9705115
11012653 120794 0 None -12 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 6 0 2 4.9 CC(C1=C(CCN(C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL355769 120794 0 None -12 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 6 0 2 4.9 CC(C1=C(CCN(C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
4715419 188717 34 None -4 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc(C2CCCN2)o1 10.1021/jm800145d
CHEMBL505086 188717 34 None -4 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 1 2 2.0 Cc1ccc(C2CCCN2)o1 10.1021/jm800145d
134272502 176284 0 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(O[C@@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4514058 176284 0 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(O[C@@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4595246 176284 0 None -2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 456 8 1 3 4.7 O=C(O[C@@H]1C[N+]2(CCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
72064 78372 14 None 2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 318 8 0 4 3.1 CCN(CC)CCOC(=O)C(c1ccccc1)N1CCCCC1 10.1016/j.bmc.2013.01.072
CHEMBL2110892 78372 14 None 2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 318 8 0 4 3.1 CCN(CC)CCOC(=O)C(c1ccccc1)N1CCCCC1 10.1016/j.bmc.2013.01.072
156017826 177834 0 None -8 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)C[C@@H]1COC[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4644285 177834 0 None -8 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 303 4 0 3 3.4 CN(C)C[C@@H]1COC[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
71461680 79506 0 None -2 2 Rat 4.7 pKi = 4.7 Binding
Inhibition of [3H]QNB binding to m3 receptor transfected with CHO cellInhibition of [3H]QNB binding to m3 receptor transfected with CHO cell
ChEMBL 245 3 0 3 2.2 CC(=O)O[C@H]1CC2CC1N(Cc1ccccc1)C2 10.1021/jm00090a006
CHEMBL2114059 79506 0 None -2 2 Rat 4.7 pKi = 4.7 Binding
Inhibition of [3H]QNB binding to m3 receptor transfected with CHO cellInhibition of [3H]QNB binding to m3 receptor transfected with CHO cell
ChEMBL 245 3 0 3 2.2 CC(=O)O[C@H]1CC2CC1N(Cc1ccccc1)C2 10.1021/jm00090a006
100 3776 58 None -8 56 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3776 58 None -8 56 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3776 58 None -8 56 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3776 58 None -8 56 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3776 58 None -8 56 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
44431376 87288 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 344 6 1 4 2.7 CN(C)C1(CNCCc2ccccc2F)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL233200 87288 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 344 6 1 4 2.7 CN(C)C1(CNCCc2ccccc2F)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
53325550 58498 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 395 9 2 4 4.9 NCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683924 58498 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 395 9 2 4 4.9 NCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
138680294 178307 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 354 3 2 1 3.9 C[N+]12CCC(CC1)[C@@H](NC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4637749 178307 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 354 3 2 1 3.9 C[N+]12CCC(CC1)[C@@H](NC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4651167 178307 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 354 3 2 1 3.9 C[N+]12CCC(CC1)[C@@H](NC(=O)Nc1ccc(F)cc1-c1ccccc1)C2 10.1021/acs.jmedchem.0c00297
155554149 175423 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 4 0 5 3.7 O=C(OCc1ccc2c(c1)OCO2)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4576768 175423 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 4 0 5 3.7 O=C(OCc1ccc2c(c1)OCO2)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
140844412 176404 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 524 8 1 3 5.7 O=C(OC1C[N+]2(CCCc3cccc(C(F)(F)F)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4441041 176404 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 524 8 1 3 5.7 O=C(OC1C[N+]2(CCCc3cccc(C(F)(F)F)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596190 176404 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 524 8 1 3 5.7 O=C(OC1C[N+]2(CCCc3cccc(C(F)(F)F)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
10597259 119231 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 402 7 2 3 3.9 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CC[C@H](F)C2)CC1 10.1021/jm0003135
CHEMBL343644 119231 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 402 7 2 3 3.9 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@H]2CC[C@H](F)C2)CC1 10.1021/jm0003135
145960466 161499 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@H](CO[C@@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
CHEMBL4128341 161499 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@H](CO[C@@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
10572658 121954 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 393 6 2 4 3.2 O=C(NC1CCN(Cc2ccncc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL359197 121954 0 None 3 3 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 393 6 2 4 3.2 O=C(NC1CCN(Cc2ccncc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
21855 84217 42 None -14 6 Human 6.7 pKi = 6.7 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1016/s0960-894x(01)00186-x
CHEMBL22108 84217 42 None -14 6 Human 6.7 pKi = 6.7 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1016/s0960-894x(01)00186-x
578009 119982 1 None - 1 Rat 5.7 pKi = 5.7 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 393 10 1 4 3.4 CN(CC#CCN1CCCC1)C(=O)CCCCCCCNC(=O)OC(C)(C)C 10.1021/jm00164a044
CHEMBL1202052 119982 1 None - 1 Rat 5.7 pKi = 5.7 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 393 10 1 4 3.4 CN(CC#CCN1CCCC1)C(=O)CCCCCCCNC(=O)OC(C)(C)C 10.1021/jm00164a044
CHEMBL350134 119982 1 None - 1 Rat 5.7 pKi = 5.7 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 393 10 1 4 3.4 CN(CC#CCN1CCCC1)C(=O)CCCCCCCNC(=O)OC(C)(C)C 10.1021/jm00164a044
11099206 120761 0 None -4 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 318 5 0 2 4.7 CC(C1=C(CCN2CCCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL355455 120761 0 None -4 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 318 5 0 2 4.7 CC(C1=C(CCN2CCCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
118719926 115754 0 None -436 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
CHEMBL3354073 115754 0 None -436 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
44593618 187435 0 None -4 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493979 187435 0 None -4 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
44299616 195685 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@@H]3[C@@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL55698 195685 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@@H]3[C@@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
10474335 194669 23 None -676 10 Human 4.7 pKi = 4.7 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 370 6 0 3 4.8 COc1cccc2c1CCCC2CCCN1CCN(C2CCCCC2)CC1 10.1038/s41586-020-2286-9
CHEMBL53325 194669 23 None -676 10 Human 4.7 pKi = 4.7 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 370 6 0 3 4.8 COc1cccc2c1CCCC2CCCN1CCN(C2CCCCC2)CC1 10.1038/s41586-020-2286-9
611101 203856 3 None -1 4 Rat 5.7 pKi = 5.7 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 380 4 2 6 0.9 NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL68771 203856 3 None -1 4 Rat 5.7 pKi = 5.7 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 380 4 2 6 0.9 NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
44337748 9363 0 None 1 2 Rat 4.7 pKi = 4.7 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
CHEMBL111529 9363 0 None 1 2 Rat 4.7 pKi = 4.7 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
168277127 190563 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 516 9 2 6 4.9 COc1cc(C(=O)O)ccc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
CHEMBL5180420 190563 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 516 9 2 6 4.9 COc1cc(C(=O)O)ccc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
118719928 115756 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354075 115756 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1 10.1021/jm501173q
44593620 187912 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496915 187912 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
137628879 160948 0 None -66 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 950 16 3 9 8.1 CCC(=O)NC1CN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)C1 10.1021/acs.jmedchem.6b01892
CHEMBL4068393 160948 0 None -66 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 950 16 3 9 8.1 CCC(=O)NC1CN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)C1 10.1021/acs.jmedchem.6b01892
CHEMBL4079233 160948 0 None -66 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 950 16 3 9 8.1 CCC(=O)NC1CN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)C1 10.1021/acs.jmedchem.6b01892
CHEMBL4115977 160948 0 None -66 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assayDisplacement of [3H]NMS from human muscarinic acetylcholine receptor M3 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
ChEMBL 950 16 3 9 8.1 CCC(=O)NC1CN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)C1 10.1021/acs.jmedchem.6b01892
16094793 83293 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsc(OCCCOCCCOCCCOc2nsnc2-c2cccnc2)n1 10.1021/jm0606995
CHEMBL219118 83293 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsc(OCCCOCCCOCCCOc2nsnc2-c2cccnc2)n1 10.1021/jm0606995
16094810 137861 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsnc1OCCCOCCCOCCCOc1nsnc1-c1cccnc1 10.1021/jm0606995
CHEMBL376295 137861 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 467 16 0 12 3.1 COc1nsnc1OCCCOCCCOCCCOc1nsnc1-c1cccnc1 10.1021/jm0606995
250 3361 8 None -56234 13 Human 5.7 pKi = 5.7 Binding
Compound was evaluated for binding affinity against Muscarinic M3 receptor using radioligand binding assayCompound was evaluated for binding affinity against Muscarinic M3 receptor using radioligand binding assay
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
5311416 3361 8 None -56234 13 Human 5.7 pKi = 5.7 Binding
Compound was evaluated for binding affinity against Muscarinic M3 receptor using radioligand binding assayCompound was evaluated for binding affinity against Muscarinic M3 receptor using radioligand binding assay
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
CHEMBL69733 3361 8 None -56234 13 Human 5.7 pKi = 5.7 Binding
Compound was evaluated for binding affinity against Muscarinic M3 receptor using radioligand binding assayCompound was evaluated for binding affinity against Muscarinic M3 receptor using radioligand binding assay
ChEMBL 502 10 1 7 5.0 COc1cc(CCCN2CCC(CC2)CCC(=O)c2cc(Cl)c(c3c2OCCO3)N)ccc1OC 10.1016/0960-894X(95)00358-Z
156011518 178314 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4637731 178314 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4651208 178314 0 None -2 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 388 5 0 2 4.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)C(c2ccccc2)(c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
10398077 9298 0 None - 1 Rat 4.7 pKi = 4.7 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heartThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heart
ChEMBL 206 2 0 3 1.6 CC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
CHEMBL111123 9298 0 None - 1 Rat 4.7 pKi = 4.7 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heartThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heart
ChEMBL 206 2 0 3 1.6 CC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
10398077 9298 0 None - 1 Rat 4.7 pKi = 4.7 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary glandThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary gland
ChEMBL 206 2 0 3 1.6 CC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
CHEMBL111123 9298 0 None - 1 Rat 4.7 pKi = 4.7 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary glandThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary gland
ChEMBL 206 2 0 3 1.6 CC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
10503358 38656 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3
ChEMBL 442 6 2 3 4.4 Cc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
CHEMBL146567 38656 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3
ChEMBL 442 6 2 3 4.4 Cc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
10497101 70440 0 None -1 3 Rat 8.7 pKi = 8.7 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 336 4 1 3 3.6 O=C(NC(c1ccccc1)c1ccccc1)OC1CN2CCC1CC2 10.1021/jm050099q
CHEMBL194628 70440 0 None -1 3 Rat 8.7 pKi = 8.7 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 336 4 1 3 3.6 O=C(NC(c1ccccc1)c1ccccc1)OC1CN2CCC1CC2 10.1021/jm050099q
90666112 109317 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 730 18 6 9 7.2 Cc1ccc(-c2ccc(O)c(Cl)c2)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c1 10.1039/C1MD00140J
CHEMBL3219044 109317 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 730 18 6 9 7.2 Cc1ccc(-c2ccc(O)c(Cl)c2)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c1 10.1039/C1MD00140J
90666116 109322 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 730 19 6 9 7.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219049 109322 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 730 19 6 9 7.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
44386115 131412 0 None 8 5 Human 8.7 pKi = 8.7 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 650 16 3 4 6.2 O=C(CCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL369062 131412 0 None 8 5 Human 8.7 pKi = 8.7 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 650 16 3 4 6.2 O=C(CCCNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCCC(=O)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
16721019 87957 0 None -1 3 Human 8.7 pKi = 8.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 362 7 2 5 2.5 CN(C)C1(CNCCC2CCC(CO)CC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234258 87957 0 None -1 3 Human 8.7 pKi = 8.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 362 7 2 5 2.5 CN(C)C1(CNCCC2CCC(CO)CC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
53372938 129276 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670828 129276 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@](O)(c1ccccc1)C1CCCC1)C2 nan
688520 35385 3 None -4 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 C[N+]1(C)CCC[C@@H](OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1016/j.bmc.2014.04.029
CHEMBL1437876 35385 3 None -4 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 C[N+]1(C)CCC[C@@H](OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1016/j.bmc.2014.04.029
CHEMBL3289390 35385 3 None -4 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 C[N+]1(C)CCC[C@@H](OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1016/j.bmc.2014.04.029
CHEMBL5271406 193657 0 None -3 5 Human 8.7 pKi = 8.7 Binding
Displacement of atropine from human muscarinic M3 receptor expressed in CHO cells incubated for 2 hrs by flow cytometric competition binding assayDisplacement of atropine from human muscarinic M3 receptor expressed in CHO cells incubated for 2 hrs by flow cytometric competition binding assay
ChEMBL 1159 27 3 10 12.8 CC1(C)C(/C=C/C=C/C=C2/N(CCCCS(=O)(=O)O)c3ccccc3C2(C)C)=[N+](CCCCCC(=O)NCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(F)c(Cl)c3)CC2)c2ccc(S(=O)(=O)[O-])cc21 10.1021/acs.jmedchem.2c01376
174174 521 49 None -2 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
260 521 49 None -2 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
320 521 49 None -2 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
CHEMBL517712 521 49 None -2 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
DB00572 521 49 None -2 14 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1016/j.bmc.2013.01.072
16115797 138130 0 None -6 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL376870 138130 0 None -6 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
56965018 77152 0 None 2 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042552 77152 0 None 2 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078967 77152 0 None 2 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL5285607 194281 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of atropine from human muscarinic M3 receptor expressed in CHO cells incubated for 2 hrs by flow cytometric competition binding assayDisplacement of atropine from human muscarinic M3 receptor expressed in CHO cells incubated for 2 hrs by flow cytometric competition binding assay
ChEMBL 1052 21 1 13 10.0 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
11006792 78893 0 None 5 5 Human 8.7 pKi = 8.7 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 648 12 2 4 5.9 O=C(CNC(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL2112961 78893 0 None 5 5 Human 8.7 pKi = 8.7 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 648 12 2 4 5.9 O=C(CNC(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NC[C@H]1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
90666102 109306 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)cc3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219032 109306 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)cc3)CC2)ccc1O 10.1039/C1MD00140J
54757772 65960 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 675 16 5 9 6.0 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Oc4nn(-c5c(O)cccc5F)c5c4CCCC5)CC3)ccc(O)c2[nH]1 10.1021/jm2007535
CHEMBL1836647 65960 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 675 16 5 9 6.0 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Oc4nn(-c5c(O)cccc5F)c5c4CCCC5)CC3)ccc(O)c2[nH]1 10.1021/jm2007535
138680039 177027 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 339 3 2 2 3.7 O=C(Nc1ccc(F)cc1-c1ccccc1)N[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4632615 177027 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 339 3 2 2 3.7 O=C(Nc1ccc(F)cc1-c1ccccc1)N[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
140844416 176582 0 None -12 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 524 8 1 3 5.7 O=C(OC1C[N+]2(CCCc3ccc(C(F)(F)F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4516342 176582 0 None -12 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 524 8 1 3 5.7 O=C(OC1C[N+]2(CCCc3ccc(C(F)(F)F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597717 176582 0 None -12 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 524 8 1 3 5.7 O=C(OC1C[N+]2(CCCc3ccc(C(F)(F)F)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL5285607 194281 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of atropine from human muscarinic M3 receptor expressed in CHO cells incubated for 2 hrs by flow cytometric competition binding assayDisplacement of atropine from human muscarinic M3 receptor expressed in CHO cells incubated for 2 hrs by flow cytometric competition binding assay
ChEMBL 1052 21 1 13 10.0 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
10621363 121664 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 406 6 2 3 4.2 Cc1cccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)c1 10.1021/jm0003135
CHEMBL358726 121664 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 406 6 2 3 4.2 Cc1cccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)c1 10.1021/jm0003135
16125620 84618 0 None 93 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 1 2 4.9 Cc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
CHEMBL222388 84618 0 None 93 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 1 2 4.9 Cc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
CHEMBL5271406 193657 0 None -3 5 Human 8.6 pKi = 8.6 Binding
Displacement of atropine from human muscarinic M3 receptor expressed in CHO cells incubated for 2 hrs by flow cytometric competition binding assayDisplacement of atropine from human muscarinic M3 receptor expressed in CHO cells incubated for 2 hrs by flow cytometric competition binding assay
ChEMBL 1159 27 3 10 12.8 CC1(C)C(/C=C/C=C/C=C2/N(CCCCS(=O)(=O)O)c3ccccc3C2(C)C)=[N+](CCCCCC(=O)NCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(F)c(Cl)c3)CC2)c2ccc(S(=O)(=O)[O-])cc21 10.1021/acs.jmedchem.2c01376
44415886 79806 0 None 74 4 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 607 8 2 4 4.3 CC(C)NC(=O)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
CHEMBL212141 79806 0 None 74 4 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 607 8 2 4 4.3 CC(C)NC(=O)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccc(F)cc1)(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm051205r
16115796 137192 0 None -3 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL375073 137192 0 None -3 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
44406316 72693 0 None 15 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 341 6 1 3 3.6 CCCCCC(O)(C#CC1(OC)CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2005.09.079
CHEMBL199821 72693 0 None 15 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 341 6 1 3 3.6 CCCCCC(O)(C#CC1(OC)CN2CCC1CC2)c1ccccc1 10.1016/j.bmcl.2005.09.079
44431382 87992 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 332 6 1 4 3.3 CN(C)C1(CNCCC2CCCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234438 87992 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 332 6 1 4 3.3 CN(C)C1(CNCCC2CCCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
53319787 58503 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 465 14 2 4 6.8 NCCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683929 58503 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 465 14 2 4 6.8 NCCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
54757668 65959 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 331 3 2 5 2.7 Oc1cccc(F)c1-n1nc(OC2CCNCC2)c2c1CCCC2 10.1021/jm2007535
CHEMBL1836646 65959 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 331 3 2 5 2.7 Oc1cccc(F)c1-n1nc(OC2CCNCC2)c2c1CCCC2 10.1021/jm2007535
1734 116 10 None 1 13 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmcl.2013.01.025
307 116 10 None 1 13 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL168067 116 10 None 1 13 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmcl.2013.01.025
319 1312 44 None -3 9 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2007.06.081
321 1312 44 None -3 9 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2007.06.081
444031 1312 44 None -3 9 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2007.06.081
784 1312 44 None -3 9 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2007.06.081
CHEMBL1346 1312 44 None -3 9 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2007.06.081
DB00496 1312 44 None -3 9 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2007.06.081
10500741 38516 0 None 1 3 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 392 6 2 3 3.8 O=C(NC1CCN(Cc2ccccc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL146464 38516 0 None 1 3 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 392 6 2 3 3.8 O=C(NC1CCN(Cc2ccccc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL5076445 214418 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CCN3C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44233190 103375 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084679 103375 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 335 5 1 2 4.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
44233192 106455 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084643 106455 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3140141 106455 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 350 5 1 1 4.4 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(CO)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
10155225 95811 0 None 2 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 3 3.6 COC1(C#CC(C#N)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL258959 95811 0 None 2 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 3 3.6 COC1(C#CC(C#N)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
44449463 96076 0 None 12 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 381 3 1 3 4.3 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL260228 96076 0 None 12 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 381 3 1 3 4.3 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
44319339 205884 0 None 44 2 Human 8.6 pKi = 8.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 386 5 1 3 4.7 O=C(c1ccccc1)N(c1ccc(O)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL83982 205884 0 None 44 2 Human 8.6 pKi = 8.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 386 5 1 3 4.7 O=C(c1ccccc1)N(c1ccc(O)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
16125373 84761 0 None 28 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 417 5 1 2 5.2 O=C1NC(c2ccccc2)(C2CCCCC2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL223267 84761 0 None 28 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 417 5 1 2 5.2 O=C1NC(c2ccccc2)(C2CCCCC2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
53326340 58504 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 479 15 2 4 7.2 NCCCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683930 58504 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 479 15 2 4 7.2 NCCCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL5282659 194144 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 465 9 2 4 5.8 NCCCCCCN1CCC(OC(=O)Nc2ccc(F)cc2-c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c01376
155541812 173026 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 5 0 3 4.1 O=C(OC1CN2CCC1CC2)N(CCc1ccc(F)cc1)c1ccccc1 10.1016/j.bmcl.2018.12.022
CHEMBL4519301 173026 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 5 0 3 4.1 O=C(OC1CN2CCC1CC2)N(CCc1ccc(F)cc1)c1ccccc1 10.1016/j.bmcl.2018.12.022
140844401 176663 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 534 8 1 3 5.5 O=C(OC1C[N+]2(CCCc3ccc(Br)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4539799 176663 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 534 8 1 3 5.5 O=C(OC1C[N+]2(CCCc3ccc(Br)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4598363 176663 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 534 8 1 3 5.5 O=C(OC1C[N+]2(CCCc3ccc(Br)cc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
10470 2471 7 None -11 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2014.04.029
1689 2471 7 None -11 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2014.04.029
4057 2471 7 None -11 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2014.04.029
CHEMBL524004 2471 7 None -11 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2014.04.029
DB04843 2471 7 None -11 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2014.04.029
16125698 84527 0 None 102 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 477 6 1 3 3.7 C[N+]1(CC(=O)c2ccccn2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222054 84527 0 None 102 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 477 6 1 3 3.7 C[N+]1(CC(=O)c2ccccn2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
44431383 87993 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 346 6 1 4 3.7 CN(C)C1(CNCCC2CCCCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234439 87993 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 346 6 1 4 3.7 CN(C)C1(CNCCC2CCCCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
16125374 84703 0 None 36 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 423 5 1 4 4.7 O=C1NC(c2cccs2)(c2cccs2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL222860 84703 0 None 36 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 423 5 1 4 4.7 O=C1NC(c2cccs2)(c2cccs2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
156011670 178293 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 391 4 1 2 5.2 C[N+]1(C)CCC(COC(=O)Nc2ccc(F)cc2-c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636887 178293 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 391 4 1 2 5.2 C[N+]1(C)CCC(COC(=O)Nc2ccc(F)cc2-c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.0c00297
CHEMBL4651086 178293 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 391 4 1 2 5.2 C[N+]1(C)CCC(COC(=O)Nc2ccc(F)cc2-c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.0c00297
16124707 138121 0 None 67 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 5 1 4 4.9 O=C1NC(c2cccs2)(c2cccs2)CN1C1CCN(Cc2cccc(F)c2)CC1 10.1021/jm061159a
CHEMBL376781 138121 0 None 67 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 5 1 4 4.9 O=C1NC(c2cccs2)(c2cccs2)CN1C1CCN(Cc2cccc(F)c2)CC1 10.1021/jm061159a
9846311 203988 12 None -1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 444 6 3 5 3.1 Nc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)n1 10.1016/s0960-894x(03)00350-0
CHEMBL69678 203988 12 None -1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 444 6 3 5 3.1 Nc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)n1 10.1016/s0960-894x(03)00350-0
16125372 84625 0 None 74 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 447 5 1 2 4.9 O=C1NC(c2ccc(F)cc2)(c2ccc(F)cc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL222424 84625 0 None 74 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 447 5 1 2 4.9 O=C1NC(c2ccc(F)cc2)(c2ccc(F)cc2)CN1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
134272441 176302 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 458 8 1 4 4.2 O=C(OC1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4442329 176302 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 458 8 1 4 4.2 O=C(OC1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4595412 176302 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 458 8 1 4 4.2 O=C(OC1C[N+]2(CCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
16086065 79768 0 None 53 4 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 622 10 3 5 3.9 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL211976 79768 0 None 53 4 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 622 10 3 5 3.9 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
9846311 203988 12 None -1 3 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 444 6 3 5 3.1 Nc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)n1 10.1021/jm0003135
CHEMBL69678 203988 12 None -1 3 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 444 6 3 5 3.1 Nc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)n1 10.1021/jm0003135
9936450 35125 0 None -3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 518 14 0 10 5.0 CN1CCC=C(c2nsnc2OCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm501173q
CHEMBL143469 35125 0 None -3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 518 14 0 10 5.0 CN1CCC=C(c2nsnc2OCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm501173q
44308912 102806 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 4 2 3 2.1 NCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)C1 10.1016/s0960-894x(03)00350-0
CHEMBL305531 102806 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 4 2 3 2.1 NCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)C1 10.1016/s0960-894x(03)00350-0
44431389 146126 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 348 6 2 5 2.3 CN(C)C1(CNCCC2CCC(O)CC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL391977 146126 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 348 6 2 5 2.3 CN(C)C1(CNCCC2CCC(O)CC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
12872437 12026 0 None -2 5 Rat 8.5 pKi = 8.5 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 338 2 0 3 3.1 C[N+]1(C)CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00403-G
CHEMBL1183585 12026 0 None -2 5 Rat 8.5 pKi = 8.5 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 338 2 0 3 3.1 C[N+]1(C)CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00403-G
CHEMBL306182 12026 0 None -2 5 Rat 8.5 pKi = 8.5 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 338 2 0 3 3.1 C[N+]1(C)CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00403-G
44406476 140499 0 None 15 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 326 3 1 4 2.2 COC1(C#CC(O)(c2ccccn2)C2CCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL381020 140499 0 None 15 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 326 3 1 4 2.2 COC1(C#CC(O)(c2ccccn2)C2CCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44431367 87953 0 None 4 3 Human 7.7 pKi = 7.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 326 6 1 4 2.6 CN(C)C1(CNCCc2ccccc2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234252 87953 0 None 4 3 Human 7.7 pKi = 7.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 326 6 1 4 2.6 CN(C)C1(CNCCc2ccccc2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
44431370 87955 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 360 6 1 4 3.2 CN(C)C1(CNCCc2ccc(Cl)cc2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234254 87955 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 360 6 1 4 3.2 CN(C)C1(CNCCc2ccc(Cl)cc2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
10214932 87198 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 300 3 0 4 3.5 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(C)C1 10.1016/j.bmcl.2007.03.047
CHEMBL232860 87198 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 300 3 0 4 3.5 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(C)C1 10.1016/j.bmcl.2007.03.047
9868297 94085 0 None 13 2 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 448 7 2 5 3.1 O=C(N[C@H]1[C@@H]2CN(CCc3ccc4c(c3)OCO4)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL249205 94085 0 None 13 2 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 448 7 2 5 3.1 O=C(N[C@H]1[C@@H]2CN(CCc3ccc4c(c3)OCO4)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
155529196 171386 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 4 0 3 4.4 Cc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
CHEMBL4462631 171386 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 4 0 3 4.4 Cc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
140844398 176337 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 534 8 1 3 5.5 O=C(OC1C[N+]2(CCCc3cccc(Br)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4470924 176337 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 534 8 1 3 5.5 O=C(OC1C[N+]2(CCCc3cccc(Br)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4595692 176337 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 534 8 1 3 5.5 O=C(OC1C[N+]2(CCCc3cccc(Br)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
71452793 79626 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 425 6 0 4 5.1 COc1ccc([S@+]([O-])c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2115127 79626 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 425 6 0 4 5.1 COc1ccc([S@+]([O-])c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
44430464 92278 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 364 3 0 4 3.6 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(Br)C1 10.1016/j.bmcl.2007.03.047
CHEMBL242823 92278 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 364 3 0 4 3.6 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(Br)C1 10.1016/j.bmcl.2007.03.047
44430467 152065 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 304 3 0 4 3.2 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(F)C1 10.1016/j.bmcl.2007.03.047
CHEMBL396761 152065 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 304 3 0 4 3.2 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(F)C1 10.1016/j.bmcl.2007.03.047
44409797 140549 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 294 6 2 4 3.8 Cc1c(NCc2ccccc2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
CHEMBL381259 140549 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 294 6 2 4 3.8 Cc1c(NCc2ccccc2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
137628788 160968 0 None -2 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 2 0 1 2.3 COc1cccc2c1CC([N+](C)(C)C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4085150 160968 0 None -2 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 2 0 1 2.3 COc1cccc2c1CC([N+](C)(C)C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116149 160968 0 None -2 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 2 0 1 2.3 COc1cccc2c1CC([N+](C)(C)C)CC2 10.1021/acs.jmedchem.7b01113
138710938 177229 0 None 7 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 353 4 2 4 3.9 N#Cc1ccc(-c2cc(F)ccc2NC(=O)OCC2CCNCC2)cc1 10.1021/acs.jmedchem.0c00297
CHEMBL4636009 177229 0 None 7 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 353 4 2 4 3.9 N#Cc1ccc(-c2cc(F)ccc2NC(=O)OCC2CCNCC2)cc1 10.1021/acs.jmedchem.0c00297
44328561 207344 0 None -4 3 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 243 3 0 3 2.5 COc1ccccc1C(=O)C1=CN2CCC1CC2 10.1016/S0960-894X(01)80824-6
CHEMBL93709 207344 0 None -4 3 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 243 3 0 3 2.5 COc1ccccc1C(=O)C1=CN2CCC1CC2 10.1016/S0960-894X(01)80824-6
2551 791 23 None -346 11 Human 4.7 pKi = 4.7 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
298 791 23 None -346 11 Human 4.7 pKi = 4.7 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
488 791 23 None -346 11 Human 4.7 pKi = 4.7 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
CHEMBL965 791 23 None -346 11 Human 4.7 pKi = 4.7 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
DB00411 791 23 None -346 11 Human 4.7 pKi = 4.7 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm020572p
137629259 160980 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 204 2 0 1 1.8 COc1cccc(C#CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4092769 160980 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 204 2 0 1 1.8 COc1cccc(C#CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116203 160980 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 204 2 0 1 1.8 COc1cccc(C#CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
9906447 195554 2 None -281 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant M3 receptorBinding affinity to human recombinant M3 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL2031738 195554 2 None -281 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant M3 receptorBinding affinity to human recombinant M3 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
CHEMBL555146 195554 2 None -281 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human recombinant M3 receptorBinding affinity to human recombinant M3 receptor
ChEMBL 351 5 0 3 4.8 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1 10.1021/jm201690h
11112362 4927 0 None -1 5 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 410 3 1 3 5.5 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(Cc5ccccc5)c34)OC21 10.1021/jm011116o
CHEMBL104804 4927 0 None -1 5 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 410 3 1 3 5.5 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(Cc5ccccc5)c34)OC21 10.1021/jm011116o
16125622 84736 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 495 6 1 3 5.5 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(OC(F)(F)F)c2)CC1 10.1021/jm061159a
CHEMBL223030 84736 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 495 6 1 3 5.5 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(OC(F)(F)F)c2)CC1 10.1021/jm061159a
16125329 84906 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 338 6 1 1 3.1 C[N+](C)(C)CCCN1CC(c2ccccc2)(c2ccccc2)NC1=O 10.1021/jm061160+
CHEMBL223724 84906 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 338 6 1 1 3.1 C[N+](C)(C)CCCN1CC(c2ccccc2)(c2ccccc2)NC1=O 10.1021/jm061160+
44593623 187856 0 None -4 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496503 187856 0 None -4 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL539373 187856 0 None -4 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
107867 2953 55 None -16 11 Human 5.7 pKi = 5.7 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm301774u
309 2953 55 None -16 11 Human 5.7 pKi = 5.7 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm301774u
CHEMBL17045 2953 55 None -16 11 Human 5.7 pKi = 5.7 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm301774u
10066972 98726 0 None -6 5 Human 5.7 pKi = 5.7 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL278074 98726 0 None -6 5 Human 5.7 pKi = 5.7 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 358 3 0 4 3.7 O=C(OC1CN2CCC1CC2)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
9968046 198140 0 None -12 4 Human 5.7 pKi = 5.7 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](/C=C/[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL57485 198140 0 None -12 4 Human 5.7 pKi = 5.7 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](/C=C/[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
10066369 120232 0 None -67 6 Human 4.7 pKi = 4.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL352375 120232 0 None -67 6 Human 4.7 pKi = 4.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
71452384 83768 0 None 4 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
CHEMBL2205816 83768 0 None 4 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
71452384 83768 0 None 4 5 Human 6.7 pKi = 6.7 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
CHEMBL2205816 83768 0 None 4 5 Human 6.7 pKi = 6.7 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
11610557 72002 0 None -8 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1CC(O)c2ccccc2C1c1ccccc1 10.1021/jm050099q
CHEMBL197588 72002 0 None -8 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1CC(O)c2ccccc2C1c1ccccc1 10.1021/jm050099q
11526446 201781 0 None -2 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@H]1c1ccsc1 10.1021/jm050099q
CHEMBL606904 201781 0 None -2 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@H]1c1ccsc1 10.1021/jm050099q
10623721 38321 0 None 16 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 457 7 3 4 3.5 NCc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
CHEMBL146307 38321 0 None 16 3 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 457 7 3 4 3.5 NCc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
156015900 178297 0 None -53 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1687 34 6 18 11.6 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCN4CCC(N5CCC(n6c(=O)[nH]c7ccccc76)CC5)CC4)cc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)c3)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)=[N+](CCCCS(=O)(=O)O)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4643273 178297 0 None -53 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1687 34 6 18 11.6 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCN4CCC(N5CCC(n6c(=O)[nH]c7ccccc76)CC5)CC4)cc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)c3)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)=[N+](CCCCS(=O)(=O)O)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651104 178297 0 None -53 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1687 34 6 18 11.6 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCN4CCC(N5CCC(n6c(=O)[nH]c7ccccc76)CC5)CC4)cc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)c3)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)=[N+](CCCCS(=O)(=O)O)c2ccccc21 10.1021/acs.jmedchem.9b02172
137630995 161117 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 4 0 2 1.6 COc1cccc(C(=O)C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4102555 161117 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 4 0 2 1.6 COc1cccc(C(=O)C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4117268 161117 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 4 0 2 1.6 COc1cccc(C(=O)C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
137630043 161013 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 4 0 1 2.4 COc1cccc(/C=C/C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4099667 161013 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 4 0 1 2.4 COc1cccc(/C=C/C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116455 161013 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 4 0 1 2.4 COc1cccc(/C=C/C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
2812 4747 101 None -22 34 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4747 101 None -22 34 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
15169865 11231 0 None -5 3 Rat 4.7 pKi = 4.7 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@H]1O[C@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL1179079 11231 0 None -5 3 Rat 4.7 pKi = 4.7 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@H]1O[C@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL59085 11231 0 None -5 3 Rat 4.7 pKi = 4.7 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@H]1O[C@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
73347826 92513 0 None -1 7 Human 5.7 pKi = 5.7 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 266 4 1 2 2.4 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)nc1 10.1016/j.bmc.2013.07.045
CHEMBL2432049 92513 0 None -1 7 Human 5.7 pKi = 5.7 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 266 4 1 2 2.4 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)nc1 10.1016/j.bmc.2013.07.045
44428745 92148 0 None -35 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cells
ChEMBL 635 23 2 6 7.9 COc1ccccc1CNCCCCCCN1CCC(CCC2CCN(CCCCCCNCc3ccccc3OC)CC2)CC1 10.1016/j.bmc.2007.01.022
CHEMBL242345 92148 0 None -35 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cells
ChEMBL 635 23 2 6 7.9 COc1ccccc1CNCCCCCCN1CCC(CCC2CCN(CCCCCCNCc3ccccc3OC)CC2)CC1 10.1016/j.bmc.2007.01.022
10033774 56516 0 None -53 4 Rat 5.7 pKi = 5.7 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 927 31 0 8 12.0 CN(CCCCCCCCN(C)CCCCCCN1CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1)CCCCCCN1CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1016/0960-894X(95)00113-8
CHEMBL163901 56516 0 None -53 4 Rat 5.7 pKi = 5.7 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 927 31 0 8 12.0 CN(CCCCCCCCN(C)CCCCCCN1CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1)CCCCCCN1CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1016/0960-894X(95)00113-8
44274469 80579 1 None -2 5 Human 4.7 pKi = 4.7 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 276 4 0 2 4.0 CN(C)CCC1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21509 80579 1 None -2 5 Human 4.7 pKi = 4.7 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 276 4 0 2 4.0 CN(C)CCC1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
57326239 77153 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042551 77153 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078974 77153 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
24894625 9746 0 None -2 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@H]1c1ccco1 10.1021/jm800145d
CHEMBL113580 9746 0 None -2 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@H]1c1ccco1 10.1021/jm800145d
CHEMBL553155 9746 0 None -2 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCC[C@H]1c1ccco1 10.1021/jm800145d
46227457 14102 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL1198075 14102 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL594801 14102 0 None -1 5 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
73346334 92512 0 None -2 7 Human 5.7 pKi = 5.7 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 265 4 1 1 3.0 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1 10.1016/j.bmc.2013.07.045
CHEMBL2432048 92512 0 None -2 7 Human 5.7 pKi = 5.7 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 265 4 1 1 3.0 c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1 10.1016/j.bmc.2013.07.045
9308 17722 21 None -234 7 Rat 4.7 pKi = 4.7 Binding
Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm00088a029
CHEMBL1255785 17722 21 None -234 7 Rat 4.7 pKi = 4.7 Binding
Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm00088a029
CHEMBL12587 17722 21 None -234 7 Rat 4.7 pKi = 4.7 Binding
Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm00088a029
CHEMBL292911 17722 21 None -234 7 Rat 4.7 pKi = 4.7 Binding
Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm00088a029
10949838 5189 0 None -72 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 4 0 6 4.4 CCOC(=O)c1c(CC)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL106218 5189 0 None -72 5 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 4 0 6 4.4 CCOC(=O)c1c(CC)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
16125158 84735 1 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 1 3 4.1 O=C1NC(c2ccccc2)(c2ccccc2)C(=O)N1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
CHEMBL223029 84735 1 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 5 1 3 4.1 O=C1NC(c2ccccc2)(c2ccccc2)C(=O)N1C1CCN(Cc2ccccc2)CC1 10.1021/jm061159a
162658112 181047 0 None -1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 393 2 0 5 4.0 CC(C)(C)OC(=O)N1CCN(CC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.bmcl.2020.127632
CHEMBL4759774 181047 0 None -1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 393 2 0 5 4.0 CC(C)(C)OC(=O)N1CCN(CC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.bmcl.2020.127632
90666108 109311 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)cc(F)c3O)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219038 109311 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)cc(F)c3O)CC2)ccc1O 10.1039/C1MD00140J
53318454 58482 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 310 3 1 3 4.0 CN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683909 58482 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 310 3 1 3 4.0 CN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
16125648 84706 0 None 44 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 477 6 1 3 3.7 C[N+]1(CC(=O)c2cccnc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222874 84706 0 None 44 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 477 6 1 3 3.7 C[N+]1(CC(=O)c2cccnc2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
155565074 175461 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 400 6 0 3 4.6 O=C(OCCCc1ccc(F)c(F)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4577453 175461 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 400 6 0 3 4.6 O=C(OCCCc1ccc(F)c(F)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
10501523 40491 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 406 6 2 3 4.2 Cc1ccccc1CN1CCC(NC(=O)C(O)(c2ccccc2)C2CCCC2)CC1 10.1021/jm0003135
CHEMBL148310 40491 0 None 5 3 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 406 6 2 3 4.2 Cc1ccccc1CN1CCC(NC(=O)C(O)(c2ccccc2)C2CCCC2)CC1 10.1021/jm0003135
10066369 120232 0 None -67 6 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL352375 120232 0 None -67 6 Human 5.7 pKi = 5.7 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
156011605 178259 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.4 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Cc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4638067 178259 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.4 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Cc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650888 178259 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.4 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Cc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
71457690 83769 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1cccnc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205817 83769 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1cccnc1 10.1016/j.bmcl.2012.08.046
16125507 166155 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 7 1 3 4.5 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CCOc2ccccc2)CC1 10.1021/jm061159a
CHEMBL426393 166155 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 7 1 3 4.5 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CCOc2ccccc2)CC1 10.1021/jm061159a
11143997 4990 0 None -32 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 408 3 1 5 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
CHEMBL105122 4990 0 None -32 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 408 3 1 5 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
9911615 99003 0 None -114 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 450 5 0 6 5.5 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(SC)cc2CCN1C3 10.1021/jm011116o
CHEMBL280220 99003 0 None -114 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 450 5 0 6 5.5 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(SC)cc2CCN1C3 10.1021/jm011116o
24894632 189395 2 None -1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc(C2CCCN2C)o1 10.1021/jm800145d
CHEMBL513277 189395 2 None -1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc(C2CCCN2C)o1 10.1021/jm800145d
44431375 87287 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 394 6 1 4 3.9 CN(C)C1(CNCCc2c(Cl)cccc2Cl)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL233199 87287 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 394 6 1 4 3.9 CN(C)C1(CNCCc2c(Cl)cccc2Cl)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
16086021 12283 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL1185033 12283 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL385229 12283 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
44627748 14062 0 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 332 4 0 1 5.4 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL1197705 14062 0 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 332 4 0 1 5.4 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL583027 14062 0 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 332 4 0 1 5.4 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
44627854 197686 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL571341 197686 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
44593620 187912 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496915 187912 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
135494454 172731 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 785 25 5 11 6.7 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
CHEMBL450986 172731 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 785 25 5 11 6.7 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O 10.1021/np050091j
122194378 123984 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 382 7 1 4 3.6 COc1ccc(CCOC(=O)NCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
CHEMBL3629537 123984 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 382 7 1 4 3.6 COc1ccc(CCOC(=O)NCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
137661377 159185 0 None -446 8 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 314 6 0 2 3.9 CCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4098720 159185 0 None -446 8 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 314 6 0 2 3.9 CCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
156010398 178212 0 None -11 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4633895 178212 0 None -11 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650561 178212 0 None -11 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)O1 10.1021/acs.jmedchem.9b02100
44422697 11820 0 None -4 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1182277 11820 0 None -4 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL227429 11820 0 None -4 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
132060812 162012 0 None -630 10 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4160064 162012 0 None -630 10 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
171578 12272 5 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 281 3 1 2 2.6 C[N+](C)(C)CC#CCOC(=O)Nc1ccc(Cl)cc1 10.1021/jm0510878
CHEMBL1184962 12272 5 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 281 3 1 2 2.6 C[N+](C)(C)CC#CCOC(=O)Nc1ccc(Cl)cc1 10.1021/jm0510878
CHEMBL380759 12272 5 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 281 3 1 2 2.6 C[N+](C)(C)CC#CCOC(=O)Nc1ccc(Cl)cc1 10.1021/jm0510878
290 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
4022 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
5926 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
CHEMBL40554 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
CHEMBL74300 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1021/jm800145d
290 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
4022 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
5926 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
CHEMBL40554 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
CHEMBL74300 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmc.2009.10.027
290 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
4022 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
5926 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
CHEMBL40554 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
CHEMBL74300 2456 6 None -7 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/j.bmcl.2014.06.020
156013387 178237 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4638935 178237 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650725 178237 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1CO[C@@H](C(c2ccccc2)c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
9817231 158212 22 None -2 7 Human 4.6 pKi = 4.6 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 282 4 0 3 4.1 CCCN1CCC=C(c2cc(-c3ccc(C)cc3)no2)C1 10.1038/s41586-020-2286-9
CHEMBL4088272 158212 22 None -2 7 Human 4.6 pKi = 4.6 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 282 4 0 3 4.1 CCCN1CCC=C(c2cc(-c3ccc(C)cc3)no2)C1 10.1038/s41586-020-2286-9
10870954 120284 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL352779 120284 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
2733638 11882 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
6508731 11882 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
8030329 11882 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
CHEMBL1182640 11882 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
CHEMBL257643 11882 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 395 12 0 1 5.3 CCN(CC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
2200 3109 46 None -11 13 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
328 3109 46 None -11 13 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
4848 3109 46 None -11 13 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
CHEMBL9967 3109 46 None -11 13 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
DB00670 3109 46 None -11 13 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00111a032
15050941 203644 0 None -1 4 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 427 4 1 5 3.1 O=C1Nc2cccnc2N(C(=O)CN2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL67381 203644 0 None -1 4 Rat 6.6 pKi = 6.6 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 427 4 1 5 3.1 O=C1Nc2cccnc2N(C(=O)CN2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/jm00111a032
44308798 204024 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 434 6 1 3 4.4 O=C(N1CCC(CCN2CCCCC2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL69904 204024 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 434 6 1 3 4.4 O=C(N1CCC(CCN2CCCCC2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
137628850 160945 0 None -1 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 1 0 1 1.8 COc1cccc2c1CC[N+](C)(C)C2 10.1021/acs.jmedchem.7b01113
CHEMBL4097248 160945 0 None -1 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 1 0 1 1.8 COc1cccc2c1CC[N+](C)(C)C2 10.1021/acs.jmedchem.7b01113
CHEMBL4115965 160945 0 None -1 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 1 0 1 1.8 COc1cccc2c1CC[N+](C)(C)C2 10.1021/acs.jmedchem.7b01113
44326538 13234 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 339 9 0 3 4.3 CCN(CC)CCOC(=O)C(CC)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL1191560 13234 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 339 9 0 3 4.3 CCN(CC)CCOC(=O)C(CC)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
16125369 166236 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 411 5 1 2 4.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCCN(Cc2ccccc2)C1 10.1021/jm061159a
CHEMBL426890 166236 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 411 5 1 2 4.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCCN(Cc2ccccc2)C1 10.1021/jm061159a
16125257 144651 0 None 7 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 350 3 1 1 3.2 C[N+]1(C)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061160+
CHEMBL390839 144651 0 None 7 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 350 3 1 1 3.2 C[N+]1(C)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061160+
10381417 68639 0 None -1 2 Rat 7.6 pKi = 7.6 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 321 5 1 2 4.6 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@H]3C2C)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
CHEMBL192061 68639 0 None -1 2 Rat 7.6 pKi = 7.6 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 321 5 1 2 4.6 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@H]3C2C)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
11718570 72173 0 None -8 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 376 3 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1Cc1ccccc1 10.1021/jm050099q
CHEMBL198065 72173 0 None -8 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 376 3 0 3 4.1 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1Cc1ccccc1 10.1021/jm050099q
53326339 58491 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 436 12 1 3 7.5 CCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683918 58491 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 436 12 1 3 7.5 CCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
44409956 76717 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 288 4 1 4 3.9 Cc1c(NC2CC2)nc(C(C)C)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL206714 76717 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 288 4 1 4 3.9 Cc1c(NC2CC2)nc(C(C)C)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
10236511 140557 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 3.9 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(C)(C)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL381333 140557 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 3.9 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(C)(C)CC1 10.1016/j.bmcl.2006.01.006
44443728 94003 0 None 25 2 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 404 6 2 3 3.9 CC(c1ccccc1)N1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
CHEMBL248809 94003 0 None 25 2 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 404 6 2 3 3.9 CC(c1ccccc1)N1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
9913341 82129 4 None -25 5 Human 7.6 pKi = 7.6 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL216927 82129 4 None -25 5 Human 7.6 pKi = 7.6 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL553058 82129 4 None -25 5 Human 7.6 pKi = 7.6 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
86720832 189943 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 476 8 2 6 4.5 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)o2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5170720 189943 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 476 8 2 6 4.5 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)o2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
168287048 191483 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 500 8 1 6 5.0 COC(=O)c1ccc(COc2cccc([C@H](NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1 10.1021/acs.jmedchem.2c00609
CHEMBL5193865 191483 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 500 8 1 6 5.0 COC(=O)c1ccc(COc2cccc([C@H](NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1 10.1021/acs.jmedchem.2c00609
44319016 206114 0 None 25 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 404 5 0 2 5.7 O=C(c1ccc(Cl)cc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL86012 206114 0 None 25 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 404 5 0 2 5.7 O=C(c1ccc(Cl)cc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
44319006 206149 0 None 12 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 384 6 0 2 4.9 O=C(Cc1ccccc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL86309 206149 0 None 12 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 384 6 0 2 4.9 O=C(Cc1ccccc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
10044685 206310 6 None 12 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 370 5 0 2 5.0 O=C(c1ccccc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL87302 206310 6 None 12 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 370 5 0 2 5.0 O=C(c1ccccc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
42853214 206431 0 None 7 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 376 5 0 3 5.1 O=C(c1cccs1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL88078 206431 0 None 7 2 Human 7.6 pKi = 7.6 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 376 5 0 3 5.1 O=C(c1cccs1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
9913341 82129 4 None -25 5 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL216927 82129 4 None -25 5 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL553058 82129 4 None -25 5 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
11748799 165387 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.3 CN(C)CCC1=C(C(C)(C)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL423831 165387 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.3 CN(C)CCC1=C(C(C)(C)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
16125618 168653 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 6 1 3 4.6 COc1ccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)cc1 10.1021/jm061159a
CHEMBL436492 168653 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 6 1 3 4.6 COc1ccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)cc1 10.1021/jm061159a
155524478 170921 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 412 7 0 4 4.5 COc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
CHEMBL4455481 170921 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 412 7 0 4 4.5 COc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
155515982 169986 0 None -100000 17 Human 4.6 pKi = 4.6 Binding
Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 169986 0 None -100000 17 Human 4.6 pKi = 4.6 Binding
Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
137629919 160985 0 None -1 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 234 3 0 1 2.5 COc1cccc2c1CCC(C[N+](C)(C)C)C2 10.1021/acs.jmedchem.7b01113
CHEMBL4095626 160985 0 None -1 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 234 3 0 1 2.5 COc1cccc2c1CCC(C[N+](C)(C)C)C2 10.1021/acs.jmedchem.7b01113
CHEMBL4116258 160985 0 None -1 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 234 3 0 1 2.5 COc1cccc2c1CCC(C[N+](C)(C)C)C2 10.1021/acs.jmedchem.7b01113
44409744 75520 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 308 6 1 4 3.9 Cc1c(NC2CC2)nc(C2CC2)nc1N(C)Cc1ccccc1 10.1016/j.bmcl.2006.01.006
CHEMBL204471 75520 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 308 6 1 4 3.9 Cc1c(NC2CC2)nc(C2CC2)nc1N(C)Cc1ccccc1 10.1016/j.bmcl.2006.01.006
44409746 76724 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 290 4 1 4 3.4 Fc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL206753 76724 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 290 4 1 4 3.4 Fc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
164616706 188491 0 None -426 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 660 14 6 8 1.7 N=C(N)NCCC[C@@H](N)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4850130 188491 0 None -426 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 660 14 6 8 1.7 N=C(N)NCCC[C@@H](N)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028391 188491 0 None -426 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 660 14 6 8 1.7 N=C(N)NCCC[C@@H](N)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
16094791 83228 0 None -6 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 443 13 0 12 1.6 COc1nsnc1OCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL218755 83228 0 None -6 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 443 13 0 12 1.6 COc1nsnc1OCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
129989 450 51 None -48 9 Rat 6.6 pKi = 6.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00046a021
8584 450 51 None -48 9 Rat 6.6 pKi = 6.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00046a021
CHEMBL43383 450 51 None -48 9 Rat 6.6 pKi = 6.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/jm00046a021
14939897 96520 0 None -199 4 Rat 6.6 pKi = 6.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1113 33 2 12 12.0 COc1ccccc1CN(CCCCCCN(C)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)Cc1ccccc1OC)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL1201994 96520 0 None -199 4 Rat 6.6 pKi = 6.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1113 33 2 12 12.0 COc1ccccc1CN(CCCCCCN(C)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)Cc1ccccc1OC)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL262913 96520 0 None -199 4 Rat 6.6 pKi = 6.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1113 33 2 12 12.0 COc1ccccc1CN(CCCCCCN(C)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)Cc1ccccc1OC)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
11833737 120313 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 Cc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
CHEMBL352966 120313 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 Cc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
101720828 97091 0 None -269 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
16147087 97091 0 None -269 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL1202002 97091 0 None -269 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL267643 97091 0 None -269 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1375 31 4 16 12.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
14939895 82090 0 None -549 4 Rat 5.6 pKi = 5.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 993 30 3 11 10.1 COc1ccccc1CNCCCCCCN(C)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL1201997 82090 0 None -549 4 Rat 5.6 pKi = 5.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 993 30 3 11 10.1 COc1ccccc1CNCCCCCCN(C)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL216629 82090 0 None -549 4 Rat 5.6 pKi = 5.6 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 993 30 3 11 10.1 COc1ccccc1CNCCCCCCN(C)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
7047822 176812 15 None 1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc([C@H]2CCCN2)c1 10.1021/jm800145d
CHEMBL461088 176812 15 None 1 5 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc([C@H]2CCCN2)c1 10.1021/jm800145d
44409787 75670 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 317 5 1 6 3.2 O=[N+]([O-])c1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL204777 75670 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 317 5 1 6 3.2 O=[N+]([O-])c1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
44420788 85113 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 452 5 1 1 5.3 C[N+]1(Cc2ccccc2)C2CCC1CC(N1CC(c3ccccc3)(c3ccccc3)NC1=O)C2 10.1021/jm061160+
CHEMBL224965 85113 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 452 5 1 1 5.3 C[N+]1(Cc2ccccc2)C2CCC1CC(N1CC(c3ccccc3)(c3ccccc3)NC1=O)C2 10.1021/jm061160+
275176 89784 1 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 355 8 1 4 3.4 CCN(CC)CCOC(=O)C(O)(c1ccccc1)c1c(C)cccc1C 10.1016/j.bmc.2013.01.072
CHEMBL2377388 89784 1 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 355 8 1 4 3.4 CCN(CC)CCOC(=O)C(O)(c1ccccc1)c1c(C)cccc1C 10.1016/j.bmc.2013.01.072
11498 2997 41 None -38 6 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1021/jm011116o
4995951 2997 41 None -38 6 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1021/jm011116o
CHEMBL59898 2997 41 None -38 6 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1021/jm011116o
47358375 180738 1 None -26 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 4 1 2 2.9 O=C(CCN1CCCc2ccccc21)NC1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4756164 180738 1 None -26 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 4 1 2 2.9 O=C(CCN1CCCc2ccccc21)NC1CCCC1 10.1016/j.bmcl.2020.127632
123603 880 29 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
2684 880 29 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
584 880 29 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
9658 880 29 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
CHEMBL168815 880 29 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1016/j.bmcl.2014.06.020
10557581 21742 0 None -489 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL1202001 21742 0 None -489 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL131913 21742 0 None -489 5 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 873 27 4 10 8.1 CN(CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
162353383 182553 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 284 4 1 4 2.2 Cn1ccc(NC(=O)CCN2CCCc3ccccc32)n1 10.1016/j.bmcl.2020.127632
CHEMBL4787944 182553 0 None -7 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 284 4 1 4 2.2 Cn1ccc(NC(=O)CCN2CCCc3ccccc32)n1 10.1016/j.bmcl.2020.127632
11057942 5548 0 None - 1 Human 4.6 pKi = 4.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 378 2 2 5 3.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(O)ccc2C1O3 10.1021/jm011116o
CHEMBL107680 5548 0 None - 1 Human 4.6 pKi = 4.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 378 2 2 5 3.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(O)ccc2C1O3 10.1021/jm011116o
44309209 204300 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 5 2 3 3.7 CC(C)(N)CC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL71483 204300 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 5 2 3 3.7 CC(C)(N)CC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
11552283 71661 0 None -2 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 3 0 4 3.8 O=C(O[C@H]1CN2CCC1CC2)C1CCc2ccccc2N1c1ccccc1 10.1021/jm050099q
CHEMBL196481 71661 0 None -2 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 3 0 4 3.8 O=C(O[C@H]1CN2CCC1CC2)C1CCc2ccccc2N1c1ccccc1 10.1021/jm050099q
90666105 109309 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(F)cc3O)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219035 109309 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(F)cc3O)CC2)ccc1O 10.1039/C1MD00140J
53372936 129275 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
CHEMBL3670827 129275 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.Radioligand Binding Assay: Radioligand binding studies were carried out with M3 receptor cell homogenates as described (Peralta et al., The EMBO Journal 6, 3923-3929, (1987)). Incubations of test ligands (or standard) with 0.2 nM [3H]4-DAMP were incubated for 120 minutes at 22 C. using human M3 receptor-expressing cell homogenates. Specific ligand binding to the receptors was defined as the difference between the total radioligand binding and the nonspecific binding determined in the presence of an excess of unlabelled ligand (10 atropine). The results were expressed as a percent of control specific binding ((measured specific binding/control specific binding)x100) obtained in the presence of various concentrations of the test compounds.
ChEMBL 344 4 1 3 3.0 C[N+]1(C)C2CCC1[C@@H](OC(=O)[C@@](O)(c1ccccc1)C1CCCC1)C2 nan
16124769 84751 0 None 23 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 6 0 2 5.3 O=C1N(C2CCN(Cc3ccccc3)CC2)CC(c2ccccc2)N1Cc1ccccc1 10.1021/jm061159a
CHEMBL223188 84751 0 None 23 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 425 6 0 2 5.3 O=C1N(C2CCN(Cc3ccccc3)CC2)CC(c2ccccc2)N1Cc1ccccc1 10.1021/jm061159a
44593625 188106 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL498358 188106 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL539120 188106 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
155521847 170663 0 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 418 5 0 3 5.3 O=C(OCCc1ccc(Cl)c(Cl)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4451770 170663 0 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 418 5 0 3 5.3 O=C(OCCc1ccc(Cl)c(Cl)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
23352279 207557 0 None -5 3 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 233 2 0 3 3.0 CC(=O)c1ccc(C2=CN3CCC2CC3)s1 10.1016/S0960-894X(01)80824-6
CHEMBL94921 207557 0 None -5 3 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 233 2 0 3 3.0 CC(=O)c1ccc(C2=CN3CCC2CC3)s1 10.1016/S0960-894X(01)80824-6
44400800 165786 0 None 1 2 Rat 5.6 pKi = 5.6 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 366 5 2 3 2.5 O=C(NCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2005.02.036
CHEMBL424832 165786 0 None 1 2 Rat 5.6 pKi = 5.6 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 366 5 2 3 2.5 O=C(NCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2005.02.036
11034265 120347 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 310 5 0 2 4.3 CC(C1=C(CCN(C)C)Cc2ccc(F)cc21)c1ccccn1 10.1021/jm020895l
CHEMBL353290 120347 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 310 5 0 2 4.3 CC(C1=C(CCN(C)C)Cc2ccc(F)cc21)c1ccccn1 10.1021/jm020895l
44593622 187772 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL495888 187772 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL556390 187772 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
11048067 5547 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 4 0 6 4.6 CCOC(=O)c1c(C)n(CC)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL107679 5547 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 4 0 6 4.6 CCOC(=O)c1c(C)n(CC)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
145961125 161522 0 None -6 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4128667 161522 0 None -6 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
162353382 181710 0 None -28 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 330 4 1 2 4.6 O=C(CCN1CCCc2ccccc21)Nc1cccc2ccccc12 10.1016/j.bmcl.2020.127632
CHEMBL4777127 181710 0 None -28 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 330 4 1 2 4.6 O=C(CCN1CCCc2ccccc21)Nc1cccc2ccccc12 10.1016/j.bmcl.2020.127632
237 204842 48 None 1 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL546257 204842 48 None 1 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL554190 204842 48 None 1 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
CHEMBL7568 204842 48 None 1 13 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 nan
145960592 161337 0 None -6 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4126071 161337 0 None -6 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 393 4 0 5 3.0 O=C(O[C@H]1CN2CCC1CC2)[C@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
44309790 203699 0 None -1 2 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 245 3 0 3 2.2 CC(=O)OC1CC2CC1CN2Cc1ccccc1 10.1021/jm00090a006
CHEMBL67700 203699 0 None -1 2 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 245 3 0 3 2.2 CC(=O)OC1CC2CC1CN2Cc1ccccc1 10.1021/jm00090a006
155523889 176500 0 None -346 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 803 21 9 9 1.8 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4454134 176500 0 None -346 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 803 21 9 9 1.8 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597014 176500 0 None -346 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 803 21 9 9 1.8 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
24894109 189004 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL509202 189004 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL551563 189004 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
92218234 120801 1 None -15 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.1 C[N+](C)(C)C[C@@H]1COCCO1 10.1016/j.bmcl.2014.06.020
CHEMBL3309718 120801 1 None -15 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.1 C[N+](C)(C)C[C@@H]1COCCO1 10.1016/j.bmcl.2014.06.020
CHEMBL3558072 120801 1 None -15 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 160 2 0 2 0.1 C[N+](C)(C)C[C@@H]1COCCO1 10.1016/j.bmcl.2014.06.020
10851461 58481 42 None 1 4 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptorDisplacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptor
ChEMBL 296 3 2 3 3.7 O=C(Nc1ccccc1-c1ccccc1)OC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL1683908 58481 42 None 1 4 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptorDisplacement of [3H]-NMS from Wistar rat salivary gland muscarinic M3 receptor
ChEMBL 296 3 2 3 3.7 O=C(Nc1ccccc1-c1ccccc1)OC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL5277670 193919 0 None -10 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 930 19 2 5 13.0 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCN3CCC(OC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
155550436 176477 0 None -346 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4569639 176477 0 None -346 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596780 176477 0 None -346 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 852 20 6 10 3.6 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
71461681 79511 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 425 6 0 4 5.1 COc1ccc([S@@+]([O-])c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2114067 79511 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 425 6 0 4 5.1 COc1ccc([S@@+]([O-])c2ccc(C(=O)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
197842 102574 3 None -8 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 326 8 0 2 3.8 CC[N+](C)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2377385 102574 3 None -8 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 326 8 0 2 3.8 CC[N+](C)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL3041160 102574 3 None -8 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 326 8 0 2 3.8 CC[N+](C)(CC)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
155553089 174081 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 394 6 0 4 4.5 COc1ccc(CCN(C(=O)OC2C[C@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4545030 174081 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 394 6 0 4 4.5 COc1ccc(CCN(C(=O)OC2C[C@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
10810094 119534 0 None 15 3 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 384 6 2 3 3.8 O=C(NC1CCN(CC2CCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL345985 119534 0 None 15 3 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 384 6 2 3 3.8 O=C(NC1CCN(CC2CCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
146025727 171661 0 None -100 27 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171661 0 None -100 27 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
71718669 86929 0 None -2 3 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 303 3 0 5 2.0 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)c3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323446 86929 0 None -2 3 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 303 3 0 5 2.0 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)c3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
44448646 11876 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 1 4.3 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCCCC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182612 11876 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 1 4.3 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCCCC1 10.1016/j.bmcl.2008.03.061
CHEMBL254586 11876 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 1 4.3 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCCCC1 10.1016/j.bmcl.2008.03.061
10969696 132079 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 334 5 0 3 3.9 CC(C1=C(CCN2CCOCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL369575 132079 0 None -1 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 334 5 0 3 3.9 CC(C1=C(CCN2CCOCC2)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
24894628 179099 0 None 1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCCC1c1ccco1 10.1021/jm800145d
CHEMBL471942 179099 0 None 1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCCC1c1ccco1 10.1021/jm800145d
CHEMBL554532 179099 0 None 1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 166 1 0 1 2.2 C[N+]1(C)CCCC1c1ccco1 10.1021/jm800145d
11101362 5093 0 None -7 5 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Cl)ccc2C1O3 10.1021/jm011116o
CHEMBL105674 5093 0 None -7 5 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Cl)ccc2C1O3 10.1021/jm011116o
44274468 80577 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 276 4 0 2 4.0 CN(C)CCC1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21508 80577 0 None -1 5 Human 4.6 pKi = 4.6 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 276 4 0 2 4.0 CN(C)CCC1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
155563061 175277 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 410 7 0 5 4.0 COc1ccc(CCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4573269 175277 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 410 7 0 5 4.0 COc1ccc(CCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1OC 10.1016/j.bmcl.2018.12.022
154734599 2486 12 None -19 12 Human 6.6 pKi = 6.6 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
327 2486 12 None -19 12 Human 6.6 pKi = 6.6 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
4108 2486 12 None -19 12 Human 6.6 pKi = 6.6 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
CHEMBL27673 2486 12 None -19 12 Human 6.6 pKi = 6.6 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm0155594
71454535 79505 0 None -1 2 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 169 1 0 3 0.6 CC(=O)O[C@@H]1CC2CC1CN2C 10.1021/jm00090a006
CHEMBL2114058 79505 0 None -1 2 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 169 1 0 3 0.6 CC(=O)O[C@@H]1CC2CC1CN2C 10.1021/jm00090a006
2200 3109 46 None -11 13 Rat 7.6 pKi = 7.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00059a009
328 3109 46 None -11 13 Rat 7.6 pKi = 7.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00059a009
4848 3109 46 None -11 13 Rat 7.6 pKi = 7.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00059a009
CHEMBL9967 3109 46 None -11 13 Rat 7.6 pKi = 7.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00059a009
DB00670 3109 46 None -11 13 Rat 7.6 pKi = 7.6 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1021/jm00059a009
10671167 121473 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3
ChEMBL 448 6 2 3 4.9 O=C(NC1CCN(CC2CCCCCC2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL358289 121473 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3Ability to inhibit binding of [3H]NMS was determined by receptor binding assay using membranes from chinese hamster ovary (CHO) cells expressing cloned Muscarinic acetylcholine receptor M3
ChEMBL 448 6 2 3 4.9 O=C(NC1CCN(CC2CCCCCC2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
11695960 72366 0 None -3 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 348 2 0 3 3.8 O=C(O[C@H]1CN2CCC1CC2)N1Cc2ccccc2C1c1ccccc1 10.1021/jm050099q
CHEMBL198669 72366 0 None -3 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 348 2 0 3 3.8 O=C(O[C@H]1CN2CCC1CC2)N1Cc2ccccc2C1c1ccccc1 10.1021/jm050099q
53318455 58505 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 556 10 5 7 4.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683931 58505 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 556 10 5 7 4.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
13981865 112785 2 None -11 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 C[N+]1(C)CCC[C@H](OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1016/j.bmc.2014.04.029
CHEMBL3289391 112785 2 None -11 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 C[N+]1(C)CCC[C@H](OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1016/j.bmc.2014.04.029
CHEMBL3306998 112785 2 None -11 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 340 4 1 3 2.7 C[N+]1(C)CCC[C@H](OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1016/j.bmc.2014.04.029
155535606 172028 0 None -77 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 1077 20 5 12 6.0 CCC(=O)NCc1cc(C(=O)NCCN2CCC(N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CC2)cc(C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)c1 10.1021/acs.jmedchem.8b01967
CHEMBL4471882 172028 0 None -77 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 1077 20 5 12 6.0 CCC(=O)NCc1cc(C(=O)NCCN2CCC(N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CC2)cc(C(=O)NCCN2CCN(CCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)CC2)c1 10.1021/acs.jmedchem.8b01967
155539713 176336 0 None -245 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4515788 176336 0 None -245 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595691 176336 0 None -245 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
289 242 12 None -257 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
9948320 242 12 None -257 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
CHEMBL1242950 242 12 None -257 14 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
155551421 173942 0 None -2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 424 7 0 5 4.5 COc1ccc(CCN(C(=O)OC2C[C@H]3CC[C@H](C2)N3C)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4541656 173942 0 None -2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 424 7 0 5 4.5 COc1ccc(CCN(C(=O)OC2C[C@H]3CC[C@H](C2)N3C)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
15629515 39127 3 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 191 1 1 2 1.8 CN(C)C1CCc2cccc(O)c2C1 10.1021/acs.jmedchem.7b01113
CHEMBL146953 39127 3 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 191 1 1 2 1.8 CN(C)C1CCc2cccc(O)c2C1 10.1021/acs.jmedchem.7b01113
44309788 102643 0 None -1 2 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CC2CC1N(C)C2 10.1021/jm00090a006
CHEMBL304551 102643 0 None -1 2 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CC2CC1N(C)C2 10.1021/jm00090a006
10871551 120485 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 340 6 0 2 5.2 CCC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
CHEMBL354523 120485 0 None -2 5 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 340 6 0 2 5.2 CCC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
44593616 193190 0 None -4 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL523518 193190 0 None -4 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
10139614 4999 0 None -19 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 462 8 1 5 5.9 CCCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL105160 4999 0 None -19 4 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 462 8 1 5 5.9 CCCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
16125531 84327 0 None 3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 412 5 1 1 4.4 C[N+]1(Cc2ccccc2)CC[C@@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL221775 84327 0 None 3 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 412 5 1 1 4.4 C[N+]1(Cc2ccccc2)CC[C@@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
71575447 86173 0 None -46 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 363 5 0 4 3.5 CN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
CHEMBL2312361 86173 0 None -46 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 363 5 0 4 3.5 CN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
11011757 59193 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 291 5 0 1 4.8 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccc1 10.1021/jm020895l
CHEMBL170221 59193 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 291 5 0 1 4.8 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccc1 10.1021/jm020895l
44593624 188105 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL498357 188105 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL554916 188105 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
109013312 180110 1 None -10 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 3 0 2 2.5 O=C(CCN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4748774 180110 1 None -10 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 258 3 0 2 2.5 O=C(CCN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
109032820 182851 1 None -7 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.1 CC1CCCN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
CHEMBL4791819 182851 1 None -7 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.1 CC1CCCN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
24894633 176876 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@H]2CCCN2C)o1 10.1021/jm800145d
CHEMBL461709 176876 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@H]2CCCN2C)o1 10.1021/jm800145d
16086031 11796 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 606 10 2 4 4.9 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL1182134 11796 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 606 10 2 4 4.9 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL214270 11796 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 606 10 2 4 4.9 O=C(NCCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
9889312 78401 0 None -4 5 Human 7.5 pKi = 7.5 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 437 6 0 5 4.4 COc1ccc([S@@+]([O-])c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2111540 78401 0 None -4 5 Human 7.5 pKi = 7.5 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 437 6 0 5 4.4 COc1ccc([S@@+]([O-])c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
44309108 103067 0 None 2 3 Human 6.5 pKi = 6.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 372 4 3 3 3.6 O=C(Nc1ccc2c(c1)CNC2)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL307554 103067 0 None 2 3 Human 6.5 pKi = 6.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 372 4 3 3 3.6 O=C(Nc1ccc2c(c1)CNC2)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
155524809 170949 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 394 5 0 5 3.7 O=C(OCCc1ccc2c(c1)OCO2)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4456047 170949 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 394 5 0 5 3.7 O=C(OCCc1ccc2c(c1)OCO2)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
44400887 70969 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 360 5 2 3 2.0 O=C(NCC#CCN1CC2CC2C1)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2005.02.036
CHEMBL195169 70969 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 360 5 2 3 2.0 O=C(NCC#CCN1CC2CC2C1)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2005.02.036
6338102 100437 1 None -20 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@@H]1O[C@@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL290723 100437 1 None -20 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@@H]1O[C@@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL59587 100437 1 None -20 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@@H]1O[C@@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
162353391 180797 0 None -4 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 282 4 1 4 2.3 O=C(CCN1CCCc2ccccc21)Nc1cccnn1 10.1016/j.bmcl.2020.127632
CHEMBL4756873 180797 0 None -4 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 282 4 1 4 2.3 O=C(CCN1CCCc2ccccc21)Nc1cccnn1 10.1016/j.bmcl.2020.127632
135 2515 43 None -22 58 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2515 43 None -22 58 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2515 43 None -22 58 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2515 43 None -22 58 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2515 43 None -22 58 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
71454526 79430 0 None 1 2 Rat 4.5 pKi = 4.5 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@@H]1C[C@@H]2C[C@H](C1)N([C@H](C)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL2113669 79430 0 None 1 2 Rat 4.5 pKi = 4.5 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@@H]1C[C@@H]2C[C@H](C1)N([C@H](C)c1ccccc1)C2 10.1021/jm00115a003
16125400 84634 0 None 35 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 494 6 1 2 4.5 C[N+]1(CC(=O)c2cccc(F)c2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222449 84634 0 None 35 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 494 6 1 2 4.5 C[N+]1(CC(=O)c2cccc(F)c2)CC[C@@H](N2CC(c3ccc(F)cc3)(c3ccc(F)cc3)NC2=O)C1 10.1021/jm061160+
10628017 21684 0 None -8 5 Rat 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 650 26 3 7 7.0 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
CHEMBL131865 21684 0 None -8 5 Rat 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 650 26 3 7 7.0 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
90666123 109330 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 752 16 6 10 6.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(OCCCN3CCC(OC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)CC3)cc2)ccc1O 10.1039/C1MD00140J
CHEMBL3219056 109330 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 752 16 6 10 6.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(OCCCN3CCC(OC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)CC3)cc2)ccc1O 10.1039/C1MD00140J
CHEMBL5268503 193543 0 None -1 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1038 20 1 13 9.7 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCN6CCC(COC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
10551354 39727 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 446 6 2 3 4.2 O=C(NC1CCN(Cc2cccc(F)c2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL147611 39727 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 446 6 2 3 4.2 O=C(NC1CCN(Cc2cccc(F)c2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
315401 89783 4 None -2 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 343 8 1 4 3.5 CCN(CC)CCSC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2377387 89783 4 None -2 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 343 8 1 4 3.5 CCN(CC)CCSC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
16125567 84729 0 None 104 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 445 5 1 2 5.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm061159a
CHEMBL223016 84729 0 None 104 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 445 5 1 2 5.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm061159a
2745 3832 42 None -21 9 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
5572 3832 42 None -21 9 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
66007 3832 42 None -21 9 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
7315 3832 42 None -21 9 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
CHEMBL1490 3832 42 None -21 9 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
DB00376 3832 42 None -21 9 Human 8.5 pKi = 8.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
10125445 75999 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to muscarinic M3 receptorsBinding affinity to muscarinic M3 receptors
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205654 75999 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Binding affinity to muscarinic M3 receptorsBinding affinity to muscarinic M3 receptors
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL5077250 214465 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3cccc(C(F)F)c3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
168275473 190413 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 490 8 2 7 3.6 Cn1nc(COc2cccc([C@@H](NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1C(=O)O 10.1021/acs.jmedchem.2c00609
CHEMBL5178217 190413 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 490 8 2 7 3.6 Cn1nc(COc2cccc([C@@H](NC(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)c2)cc1C(=O)O 10.1021/acs.jmedchem.2c00609
168276300 190485 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 487 8 2 6 4.3 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)nc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5179380 190485 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 487 8 2 6 4.3 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)nc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
69058946 106448 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084658 106448 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3140110 106448 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membraneDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cell membrane
ChEMBL 336 4 1 1 4.3 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
10125445 75999 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2007.03.047
CHEMBL205654 75999 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2007.03.047
118737354 119034 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 703 12 6 8 5.8 Cc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426701 119034 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 703 12 6 8 5.8 Cc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
2705 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.09.079
360 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.09.079
443879 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.09.079
CHEMBL1382 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.09.079
DB01036 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.09.079
10269504 134348 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL371734 134348 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL5289601 194449 0 None -5 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 973 22 2 5 14.1 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCCCN3CCC(COC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
10125445 75999 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2007.03.047
CHEMBL205654 75999 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2007.03.047
10125445 75999 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205654 75999 0 None 3 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 4 3.6 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
9910802 120984 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 434 6 2 4 4.2 O=C(NC1CCN(Cc2ccsc2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL356505 120984 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 434 6 2 4 4.2 O=C(NC1CCN(Cc2ccsc2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
44385809 61436 0 None 22 5 Human 8.5 pKi = 8.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 636 15 3 4 5.8 O=C(CCCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
CHEMBL177040 61436 0 None 22 5 Human 8.5 pKi = 8.5 Binding
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3
ChEMBL 636 15 3 4 5.8 O=C(CCCNC(=O)CNC(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1)NCC1CCCN(CC2CCCCC2)C1 10.1021/jm010480k
44308733 102163 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 380 5 2 3 3.3 CC1(CCN)CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL302809 102163 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 380 5 2 3 3.3 CC1(CCN)CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
44431381 148997 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 318 6 1 4 2.9 CN(C)C1(CNCCC2CCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL394254 148997 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 318 6 1 4 2.9 CN(C)C1(CNCCC2CCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
44311762 163448 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 440 6 1 5 4.0 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCNCC2)CC1 10.1016/s0960-894x(00)00457-1
CHEMBL420008 163448 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 440 6 1 5 4.0 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCNCC2)CC1 10.1016/s0960-894x(00)00457-1
11561621 201780 0 None -3 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccsc1 10.1021/jm050099q
CHEMBL606903 201780 0 None -3 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccsc1 10.1021/jm050099q
11798126 41942 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 458 7 2 4 4.1 COc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
CHEMBL149484 41942 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 458 7 2 4 4.1 COc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
10693031 120961 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 412 6 2 4 4.2 Cc1cc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)cs1 10.1021/jm0003135
CHEMBL356305 120961 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 412 6 2 4 4.2 Cc1cc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)cs1 10.1021/jm0003135
11501540 133578 0 None -3 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1c1cccs1 10.1021/jm050099q
CHEMBL371293 133578 0 None -3 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 4 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1c1cccs1 10.1021/jm050099q
2705 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
360 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
443879 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
CHEMBL1382 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
DB01036 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2007.11.022
2705 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2010.10.132
360 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2010.10.132
443879 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2010.10.132
CHEMBL1382 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2010.10.132
DB01036 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2010.10.132
2705 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/jm2007535
360 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/jm2007535
443879 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/jm2007535
CHEMBL1382 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/jm2007535
DB01036 3813 64 None -1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/jm2007535
2705 3813 64 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
360 3813 64 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
443879 3813 64 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
CHEMBL1382 3813 64 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
DB01036 3813 64 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting methodDisplacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1021/acs.jmedchem.8b00041
10834711 121384 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 398 6 2 4 3.9 O=C(NC1CCN(Cc2ccsc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL358193 121384 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 398 6 2 4 3.9 O=C(NC1CCN(Cc2ccsc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
42596929 77159 0 None -4 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042404 77159 0 None -4 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079021 77159 0 None -4 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)CC1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
9827782 103526 0 None -41 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 512 7 0 6 4.9 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCN(C(=O)OCC)CC2)CC1 10.1016/s0960-894x(00)00457-1
CHEMBL308566 103526 0 None -41 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cellsBinding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
ChEMBL 512 7 0 6 4.9 C=C(c1ccc(S(=O)(=O)c2ccc(OC)cc2)cc1)C1CCN(C2CCN(C(=O)OCC)CC2)CC1 10.1016/s0960-894x(00)00457-1
9799291 160096 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 366 5 2 3 2.9 NCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL410890 160096 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 366 5 2 3 2.9 NCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
90666103 109307 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cccc(O)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219033 109307 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cccc(O)c3)CC2)ccc1O 10.1039/C1MD00140J
44554514 123961 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 692 18 5 9 5.9 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)c5ccccc5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629356 123961 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 692 18 5 9 5.9 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)c5ccccc5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
44609903 123964 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc([C@](O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629359 123964 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc([C@](O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
16086004 139212 0 None 77 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 608 9 3 5 3.5 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL378885 139212 0 None 77 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 608 9 3 5 3.5 O=C(NC[C@@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
155551383 176600 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 582 8 1 3 5.3 O=C(OC1C[N+]2(CCCc3cccc(I)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4541647 176600 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 582 8 1 3 5.3 O=C(OC1C[N+]2(CCCc3cccc(I)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597851 176600 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 582 8 1 3 5.3 O=C(OC1C[N+]2(CCCc3cccc(I)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
10812455 39757 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 428 6 2 3 4.1 O=C(NC1CCN(Cc2ccccc2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL147653 39757 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 428 6 2 3 4.1 O=C(NC1CCN(Cc2ccccc2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
16065268 67899 0 None 2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 456 9 1 3 5.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2ccccc2)CC1 10.1021/jm200884j
CHEMBL1910849 67899 0 None 2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 456 9 1 3 5.6 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CCC(Oc2ccccc2)CC1 10.1021/jm200884j
164617537 185189 0 None -100 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 654 15 5 8 5.4 O=C(N[C@H](c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4857743 185189 0 None -100 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 654 15 5 8 5.4 O=C(N[C@H](c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164627100 186535 0 None -25 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 739 13 6 9 5.8 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmcl.2021.127975
CHEMBL4878138 186535 0 None -25 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptorDisplacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
ChEMBL 739 13 6 9 5.8 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmcl.2021.127975
90209394 191061 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 493 8 2 7 4.3 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)O)cs2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5187593 191061 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 493 8 2 7 4.3 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)O)cs2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
168287089 191527 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 504 8 2 5 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)c(F)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5194569 191527 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 504 8 2 5 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)c(F)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
10269504 134348 0 None 6 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
CHEMBL371734 134348 0 None 6 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO cells
ChEMBL 353 3 1 3 3.6 CO[C@]1(C#C[C@@](O)(c2ccccc2)C2CCCCC2)CN2CCC1CC2 10.1016/j.bmcl.2008.03.024
44318928 205740 0 None 28 2 Human 8.4 pKi = 8.4 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 400 6 0 3 5.0 COc1ccc(N(C(=O)c2ccccc2)C2CCN(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00487-0
CHEMBL82859 205740 0 None 28 2 Human 8.4 pKi = 8.4 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 400 6 0 3 5.0 COc1ccc(N(C(=O)c2ccccc2)C2CCN(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00487-0
44319043 206036 0 None 17 2 Human 8.4 pKi = 8.4 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 410 5 0 3 5.7 O=C(c1cccs1)N(c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL85391 206036 0 None 17 2 Human 8.4 pKi = 8.4 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 410 5 0 3 5.7 O=C(c1cccs1)N(c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
2774 3839 95 None -2 10 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
5593 3839 95 None -2 10 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
7319 3839 95 None -2 10 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
CHEMBL1200604 3839 95 None -2 10 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB00809 3839 95 None -2 10 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
DB01199 3839 95 None -2 10 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 nan
2733619 11879 8 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 451 16 0 1 6.8 CCCCN(CCCC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
6508725 11879 8 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 451 16 0 1 6.8 CCCCN(CCCC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
CHEMBL1182634 11879 8 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 451 16 0 1 6.8 CCCCN(CCCC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
CHEMBL257431 11879 8 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 451 16 0 1 6.8 CCCCN(CCCC)c1ccc(/C=C/c2cc[n+](CCC[N+](CC)(CC)CC)cc2)cc1 10.1016/j.bmcl.2007.11.022
138710717 177998 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1ccccc1Cl)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4646717 177998 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1ccccc1Cl)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
10574041 39792 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 418 6 2 4 3.7 O=C(NC1CCN(Cc2ccoc2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL147695 39792 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 418 6 2 4 3.7 O=C(NC1CCN(Cc2ccoc2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
156021441 178130 0 None -6 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4648939 178130 0 None -6 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1COC[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/acs.jmedchem.9b02100
155562882 175209 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 350 5 0 3 4.0 O=C(OCCc1ccccc1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4571841 175209 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 350 5 0 3 4.0 O=C(OCCc1ccccc1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
44318930 106145 0 None -6 4 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 251 2 0 3 2.7 CN1C2CCCC1C(OC(=O)C1CCCCC1)C2 10.1021/jm9904001
CHEMBL313738 106145 0 None -6 4 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 251 2 0 3 2.7 CN1C2CCCC1C(OC(=O)C1CCCCC1)C2 10.1021/jm9904001
10235 2656 1 None -1230 6 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M3 receptor (unknown origin)Inhibition of muscarinic M3 receptor (unknown origin)
ChEMBL 433 6 4 8 2.1 OC[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC(C1CCC1)C1CCC1 10.1021/acs.jmedchem.8b01662
137553161 2656 1 None -1230 6 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M3 receptor (unknown origin)Inhibition of muscarinic M3 receptor (unknown origin)
ChEMBL 433 6 4 8 2.1 OC[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC(C1CCC1)C1CCC1 10.1021/acs.jmedchem.8b01662
CHEMBL4470080 2656 1 None -1230 6 Human 5.5 pKi = 5.5 Binding
Inhibition of muscarinic M3 receptor (unknown origin)Inhibition of muscarinic M3 receptor (unknown origin)
ChEMBL 433 6 4 8 2.1 OC[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC(C1CCC1)C1CCC1 10.1021/acs.jmedchem.8b01662
137640201 156937 2 None -2398 13 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156937 2 None -2398 13 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
44593617 187407 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493795 187407 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
10373706 57379 0 None -60 4 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 959 31 2 10 10.2 CN(CCCCCCCCN(C)CCCCCCN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1)CCCCCCN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1016/0960-894X(95)00113-8
CHEMBL165220 57379 0 None -60 4 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 959 31 2 10 10.2 CN(CCCCCCCCN(C)CCCCCCN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1)CCCCCCN1CCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1016/0960-894X(95)00113-8
441383 20301 57 None -6 17 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 20301 57 None -6 17 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
11808946 120610 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 6 0 2 4.5 CCC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL354678 120610 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 6 0 2 4.5 CCC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
135430667 4926 0 None -50 5 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 402 2 1 6 4.3 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(-c5nc(C)no5)c34)OC21 10.1021/jm011116o
CHEMBL104803 4926 0 None -50 5 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 402 2 1 6 4.3 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(-c5nc(C)no5)c34)OC21 10.1021/jm011116o
15157139 99783 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 331 8 0 3 4.4 CN(C)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL285440 99783 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 331 8 0 3 4.4 CN(C)CCCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
10410916 94041 0 None 9 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 438 7 2 3 4.0 O=C(N[C@H]1[C@@H]2CN(CCc3ccc(Cl)cc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL249007 94041 0 None 9 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 438 7 2 3 4.0 O=C(N[C@H]1[C@@H]2CN(CCc3ccc(Cl)cc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
11808040 168371 0 None -2 6 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 4 0 2 3.8 CC(C1=C(CN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL434684 168371 0 None -2 6 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 4 0 2 3.8 CC(C1=C(CN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
25034182 172560 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic acetylcholine M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic acetylcholine M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL448870 172560 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic acetylcholine M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic acetylcholine M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
CHEMBL540359 172560 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic acetylcholine M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic acetylcholine M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 589 10 5 6 4.3 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3cccc(O)c3)C2)cc1 10.1021/jm800634k
44319017 206286 0 None 19 2 Human 7.5 pKi = 7.5 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 448 5 0 2 5.8 O=C(c1ccc(Br)cc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL87132 206286 0 None 19 2 Human 7.5 pKi = 7.5 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 448 5 0 2 5.8 O=C(c1ccc(Br)cc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
44443722 154896 0 None 29 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 404 6 2 3 3.7 O=C(N[C@H]1[C@@H]2CN(Cc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL400953 154896 0 None 29 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 404 6 2 3 3.7 O=C(N[C@H]1[C@@H]2CN(Cc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.06.081
16125325 84544 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 336 3 1 1 2.8 C[N+]1(C)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222090 84544 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 336 3 1 1 2.8 C[N+]1(C)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
535891 119847 2 None - 1 Rat 5.5 pKi = 5.5 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 279 8 1 3 1.5 CN(CC#CCN1CCCC1)C(=O)CCCCCCN 10.1021/jm00164a044
CHEMBL1202131 119847 2 None - 1 Rat 5.5 pKi = 5.5 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 279 8 1 3 1.5 CN(CC#CCN1CCCC1)C(=O)CCCCCCN 10.1021/jm00164a044
CHEMBL348946 119847 2 None - 1 Rat 5.5 pKi = 5.5 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 279 8 1 3 1.5 CN(CC#CCN1CCCC1)C(=O)CCCCCCN 10.1021/jm00164a044
71575122 86184 0 None -134 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 377 6 0 4 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
CHEMBL2312376 86184 0 None -134 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 377 6 0 4 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
12488 1644 56 None -8 23 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1644 56 None -8 23 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1644 56 None -8 23 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1644 56 None -8 23 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
16125327 84722 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 412 5 1 1 4.4 C[N+]1(Cc2ccccc2)CC[C@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222975 84722 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 412 5 1 1 4.4 C[N+]1(Cc2ccccc2)CC[C@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
44409749 76515 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 350 4 1 4 4.1 Brc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL206127 76515 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 350 4 1 4 4.1 Brc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
44409962 77286 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 320 4 1 4 3.8 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCc2ccccc2C1 10.1016/j.bmcl.2006.01.006
CHEMBL208299 77286 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 320 4 1 4 3.8 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCc2ccccc2C1 10.1016/j.bmcl.2006.01.006
44409760 138637 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 5 2 4 4.0 Cc1c(NC2CCCCC2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
CHEMBL377728 138637 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 5 2 4 4.0 Cc1c(NC2CCCCC2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
44418764 82130 0 None -8 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
CHEMBL216928 82130 0 None -8 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
10109893 82136 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
CHEMBL216983 82136 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
CHEMBL544840 82136 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 373 13 1 9 0.7 CN1CCC=C(c2nsnc2OCCOCCOCCOCCO)C1 10.1021/jm0606995
11131099 120235 0 None -3 5 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 3 4.2 COc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
CHEMBL352404 120235 0 None -3 5 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 3 4.2 COc1ccc2c(c1)C(C(C)c1ccccn1)=C(CCN(C)C)C2 10.1021/jm020895l
10337773 101558 0 None -79 10 Human 4.5 pKi = 4.5 Binding
Binding affinity against Muscarinic M3 receptorBinding affinity against Muscarinic M3 receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
CHEMBL298612 101558 0 None -79 10 Human 4.5 pKi = 4.5 Binding
Binding affinity against Muscarinic M3 receptorBinding affinity against Muscarinic M3 receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
162353372 181363 0 None -8 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 2.2 O=C(CCN1CCCc2ccccc21)N1CCCCC1CO 10.1016/j.bmcl.2020.127632
CHEMBL4763422 181363 0 None -8 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 2.2 O=C(CCN1CCCc2ccccc21)N1CCCCC1CO 10.1016/j.bmcl.2020.127632
57326146 77158 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042403 77158 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079020 77158 0 None -1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@@H](c2ccccc2)O1 10.1021/jm2013216
2750 204038 76 None -1 12 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 204038 76 None -1 12 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
53319788 58512 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 624 17 5 6 5.4 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)C1 10.1016/j.bmcl.2011.01.043
CHEMBL1683939 58512 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 624 17 5 6 5.4 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)C1 10.1016/j.bmcl.2011.01.043
44430461 168327 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 314 3 0 4 3.9 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(C)(C)C1 10.1016/j.bmcl.2007.03.047
CHEMBL434388 168327 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 314 3 0 4 3.9 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(C)(C)C1 10.1016/j.bmcl.2007.03.047
44409653 76486 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 270 4 1 4 3.0 Cc1c(NC2CC2)nc(C2CC2)nc1N1CC=CCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205992 76486 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 270 4 1 4 3.0 Cc1c(NC2CC2)nc(C2CC2)nc1N1CC=CCC1 10.1016/j.bmcl.2006.01.006
44409765 138638 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 3.9 Cc1c(NC2CC2)nc([C@@H]2C[C@H]2C)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL377729 138638 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 3.9 Cc1c(NC2CC2)nc([C@@H]2C[C@H]2C)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
10830843 203940 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 4 3 3 2.2 O=C(NC1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL69383 203940 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 4 3 3 2.2 O=C(NC1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
44409557 140982 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 5 2.4 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(=O)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL382374 140982 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 5 2.4 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(=O)CC1 10.1016/j.bmcl.2006.01.006
10421982 206018 0 None -5 4 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 245 2 0 3 2.5 CN1C2CCCC1C(OC(=O)c1ccccc1)C2 10.1021/jm9904001
CHEMBL85190 206018 0 None -5 4 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 245 2 0 3 2.5 CN1C2CCCC1C(OC(=O)c1ccccc1)C2 10.1021/jm9904001
578008 56404 1 None - 1 Rat 5.5 pKi = 5.5 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 379 9 1 4 3.0 CN(CC#CCN1CCCC1)C(=O)CCCCCCNC(=O)OC(C)(C)C 10.1021/jm00164a044
CHEMBL1202048 56404 1 None - 1 Rat 5.5 pKi = 5.5 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 379 9 1 4 3.0 CN(CC#CCN1CCCC1)C(=O)CCCCCCNC(=O)OC(C)(C)C 10.1021/jm00164a044
CHEMBL163202 56404 1 None - 1 Rat 5.5 pKi = 5.5 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 379 9 1 4 3.0 CN(CC#CCN1CCCC1)C(=O)CCCCCCNC(=O)OC(C)(C)C 10.1021/jm00164a044
2274 3151 58 None -21 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3151 58 None -21 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3151 58 None -21 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3151 58 None -21 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3151 58 None -21 32 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
2551 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44627855 197348 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569212 197348 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCC[C@@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
44593624 188105 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL498357 188105 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL554916 188105 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
44593627 193275 0 None -2 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524071 193275 0 None -2 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL541671 193275 0 None -2 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
162353375 179871 0 None -9 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 4 0 3 1.7 COC1CN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
CHEMBL4745885 179871 0 None -9 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 274 4 0 3 1.7 COC1CN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
162353384 181066 0 None -6 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC1CO 10.1016/j.bmcl.2020.127632
CHEMBL4760037 181066 0 None -6 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC1CO 10.1016/j.bmcl.2020.127632
46227461 14104 0 None 1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198077 14104 0 None 1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL594803 14104 0 None 1 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
122194372 123980 0 None 2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 352 6 1 3 3.0 COc1ccc(CCNC(=O)C2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
CHEMBL3629532 123980 0 None 2 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 352 6 1 3 3.0 COc1ccc(CCNC(=O)C2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
4841 67397 5 None -3 5 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
CHEMBL1889399 67397 5 None -3 5 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
CHEMBL1909073 67397 5 None -3 5 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
44443732 94209 0 None 41 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 382 7 2 3 3.5 CC(C)=CCCN1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
CHEMBL250030 94209 0 None 41 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 382 7 2 3 3.5 CC(C)=CCCN1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
44379508 58134 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 664 9 1 4 6.6 CCN(CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1)C(=O)c1cccc(I)c1 10.1016/S0960-894X(97)00109-1
CHEMBL168145 58134 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 664 9 1 4 6.6 CCN(CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1)C(=O)c1cccc(I)c1 10.1016/S0960-894X(97)00109-1
44627742 198354 0 None -2 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 323 4 0 2 5.8 CN1CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL576707 198354 0 None -2 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 323 4 0 2 5.8 CN1CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
9998202 69137 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
CHEMBL192485 69137 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
14939893 9502 0 None -112 5 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 621 24 3 7 6.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
CHEMBL112244 9502 0 None -112 5 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 621 24 3 7 6.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
2719 914 74 None -3 11 Human 5.5 pKi = 5.5 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
5535 914 74 None -3 11 Human 5.5 pKi = 5.5 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
607 914 74 None -3 11 Human 5.5 pKi = 5.5 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
CHEMBL76 914 74 None -3 11 Human 5.5 pKi = 5.5 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
DB00608 914 74 None -3 11 Human 5.5 pKi = 5.5 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC 10.1038/s41586-020-2286-9
10315426 101021 0 None -10 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@@H]3[C@@H](C#C[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL294663 101021 0 None -10 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@@H]3[C@@H](C#C[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
162353369 180771 0 None -2 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC(O)CC1 10.1016/j.bmcl.2020.127632
CHEMBL4756442 180771 0 None -2 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC(O)CC1 10.1016/j.bmcl.2020.127632
24894516 172684 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@@H]2CCCN2C)o1 10.1021/jm800145d
CHEMBL450463 172684 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 165 1 0 2 2.4 Cc1ccc([C@@H]2CCCN2C)o1 10.1021/jm800145d
16125535 85089 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 324 5 1 1 2.7 C[N+](C)(C)CCN1CC(c2ccccc2)(c2ccccc2)NC1=O 10.1021/jm061160+
CHEMBL224784 85089 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 324 5 1 1 2.7 C[N+](C)(C)CCN1CC(c2ccccc2)(c2ccccc2)NC1=O 10.1021/jm061160+
36381 12910 5 None 1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmcl.2012.08.046
CHEMBL1189234 12910 5 None 1 6 Human 6.5 pKi = 6.5 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmcl.2012.08.046
36381 12910 5 None 1 6 Human 6.5 pKi = 6.5 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmc.2013.07.045
CHEMBL1189234 12910 5 None 1 6 Human 6.5 pKi = 6.5 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 265 2 1 2 1.9 OC12C3C4CC5C6C4C1C6C(C53)N2Cc1ccccc1 10.1016/j.bmc.2013.07.045
118719930 115758 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 470 17 1 3 6.7 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354077 115758 0 None -3 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 470 17 1 3 6.7 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCCCCCO)CC1 10.1021/jm501173q
10225881 107594 0 None -112 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 450 6 1 5 5.9 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
CHEMBL318995 107594 0 None -112 5 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 450 6 1 5 5.9 CCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(SC)ccc2C1O3 10.1021/jm011116o
44337776 111163 0 None -1 2 Rat 5.5 pKi = 5.5 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@H]1CC2CC(C1)N(C(C)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL326453 111163 0 None -1 2 Rat 5.5 pKi = 5.5 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@H]1CC2CC(C1)N(C(C)c1ccccc1)C2 10.1021/jm00115a003
12963076 196602 4 None -8128 7 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL564226 196602 4 None -8128 7 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 292 5 0 2 4.1 C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
24865895 95976 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL259662 95976 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL390842 95976 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
11523051 96260 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 218 1 0 2 0.7 C[C@@H]1O[C@H]([C@@H]2CCC[N+]2(C)C)C[S@@+]1[O-] 10.1021/jm0510878
CHEMBL2093084 96260 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 218 1 0 2 0.7 C[C@@H]1O[C@H]([C@@H]2CCC[N+]2(C)C)C[S@@+]1[O-] 10.1021/jm0510878
CHEMBL261194 96260 0 None -2 5 Human 4.5 pKi = 4.5 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 218 1 0 2 0.7 C[C@@H]1O[C@H]([C@@H]2CCC[N+]2(C)C)C[S@@+]1[O-] 10.1021/jm0510878
44576913 193290 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 336 4 0 2 3.3 C[N+](C)(C)C[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524186 193290 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 336 4 0 2 3.3 C[N+](C)(C)C[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL557808 193290 0 None -1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 336 4 0 2 3.3 C[N+](C)(C)C[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
2551 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44593621 193273 0 None -2 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524061 193273 0 None -2 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
15050949 203953 0 None -3 3 Rat 5.5 pKi = 5.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 641 10 3 8 4.2 CC(C)(C)OC(=O)NCCCCNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
CHEMBL69458 203953 0 None -3 3 Rat 5.5 pKi = 5.5 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 641 10 3 8 4.2 CC(C)(C)OC(=O)NCCCCNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
44400375 69145 0 None 2 2 Rat 7.5 pKi = 7.5 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 367 5 1 4 3.0 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2005.02.036
CHEMBL192537 69145 0 None 2 2 Rat 7.5 pKi = 7.5 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 367 5 1 4 3.0 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2005.02.036
9842753 201789 0 None 1 3 Rat 7.5 pKi = 7.5 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1C[C@@H](O)c2ccccc2[C@@H]1c1ccccc1 10.1021/jm050099q
CHEMBL606963 201789 0 None 1 3 Rat 7.5 pKi = 7.5 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1C[C@@H](O)c2ccccc2[C@@H]1c1ccccc1 10.1021/jm050099q
155567380 176384 0 None -446 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 981 20 7 10 4.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4589047 176384 0 None -446 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 981 20 7 10 4.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596064 176384 0 None -446 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 981 20 7 10 4.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
155520267 170420 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 356 5 0 3 4.1 CN1CCCC(OC(=O)N(CCc2ccc(F)cc2)c2ccccc2)C1 10.1016/j.bmcl.2018.12.022
CHEMBL4448667 170420 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 356 5 0 3 4.1 CN1CCCC(OC(=O)N(CCc2ccc(F)cc2)c2ccccc2)C1 10.1016/j.bmcl.2018.12.022
16125503 84654 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 417 5 1 2 5.0 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CC2CCCCC2)CC1 10.1021/jm061159a
CHEMBL222527 84654 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 417 5 1 2 5.0 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(CC2CCCCC2)CC1 10.1021/jm061159a
156012936 178272 0 None -5 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4639004 178272 0 None -5 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650969 178272 0 None -5 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
162353386 180956 0 None -3 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 3 0 2 3.6 C[C@H]1CCC[C@@H](C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
CHEMBL4758635 180956 0 None -3 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 3 0 2 3.6 C[C@H]1CCC[C@@H](C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
44422692 11821 0 None -5 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1182296 11821 0 None -5 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL228144 11821 0 None -5 5 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
44446841 12306 0 None -2 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL1185281 12306 0 None -2 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL404557 12306 0 None -2 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
122194380 123985 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 381 7 2 3 3.2 COc1ccc(CCNC(=O)NCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
CHEMBL3629539 123985 0 None 1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 381 7 2 3 3.2 COc1ccc(CCNC(=O)NCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
16125640 84713 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 486 10 1 3 4.3 COCC[N+]1(CCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222917 84713 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 486 10 1 3 4.3 COCC[N+]1(CCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
2551 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2398 951 62 None -1 29 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 951 62 None -1 29 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 951 62 None -1 29 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 951 62 None -1 29 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 951 62 None -1 29 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
1971 2846 38 None -4 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2846 38 None -4 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2846 38 None -4 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2846 38 None -4 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2846 38 None -4 30 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
90666122 109329 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 738 15 6 10 5.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(OCCN3CCC(OC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)CC3)cc2)ccc1O 10.1039/C1MD00140J
CHEMBL3219055 109329 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 738 15 6 10 5.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(OCCN3CCC(OC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)CC3)cc2)ccc1O 10.1039/C1MD00140J
44627744 14008 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 348 4 1 2 4.5 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL1197389 14008 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 348 4 1 2 4.5 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL569729 14008 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 348 4 1 2 4.5 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
71457691 83770 0 None -1 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccccc1CN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205823 83770 0 None -1 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 295 3 1 3 2.0 COc1ccccc1CN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
53414666 159277 8 None -3 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 4 1 3 1.2 c1cncc(COCC2CCNC2)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4099673 159277 8 None -3 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 4 1 3 1.2 c1cncc(COCC2CCNC2)c1 10.1021/acs.jmedchem.7b01113
574782 102124 2 None 1 3 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 397 3 1 6 2.3 CSc1ccc2c(c1)C(=O)Nc1cccnc1N2C(=O)CN1CCN(C)CC1 10.1021/jm00111a032
CHEMBL302557 102124 2 None 1 3 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 397 3 1 6 2.3 CSc1ccc2c(c1)C(=O)Nc1cccnc1N2C(=O)CN1CCN(C)CC1 10.1021/jm00111a032
44448380 11883 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 436 7 1 1 5.0 C[N+]1(C)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182644 11883 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 436 7 1 1 5.0 C[N+]1(C)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL257804 11883 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 436 7 1 1 5.0 C[N+]1(C)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
44422699 11819 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1182272 11819 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL227378 11819 0 None -5 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
15050948 102790 0 None -3 4 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 513 7 3 7 1.8 NCCNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
CHEMBL305403 102790 0 None -3 4 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 513 7 3 7 1.8 NCCNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
44400762 70539 0 None 2 2 Rat 6.4 pKi = 6.4 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 396 5 2 3 2.3 O=C(NCC#CCN1CC2CC2C1)C(O)(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2005.02.036
CHEMBL194870 70539 0 None 2 2 Rat 6.4 pKi = 6.4 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 396 5 2 3 2.3 O=C(NCC#CCN1CC2CC2C1)C(O)(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2005.02.036
9998202 69137 0 None 2 2 Rat 7.4 pKi = 7.4 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
CHEMBL192485 69137 0 None 2 2 Rat 7.4 pKi = 7.4 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
4601 206724 35 None -1 17 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 206724 35 None -1 17 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 206724 35 None -1 17 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
71449148 79509 0 None -4 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 436 6 0 4 5.5 COc1ccc([S@@+]([O-])c2ccc(C(C#N)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2114064 79509 0 None -4 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 436 6 0 4 5.5 COc1ccc([S@@+]([O-])c2ccc(C(C#N)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
156014205 178268 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4635385 178268 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650957 178268 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
162645520 183604 0 None -89 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 1117 25 4 11 9.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4742721 183604 0 None -89 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 1117 25 4 11 9.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4802414 183604 0 None -89 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 1117 25 4 11 9.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
122194374 123982 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 367 7 0 4 3.8 COc1ccc(CCC(=O)OCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
CHEMBL3629534 123982 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 367 7 0 4 3.8 COc1ccc(CCC(=O)OCC2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
71716836 86925 0 None -4 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 348 4 0 7 1.9 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)c3ccccc3[N+](=O)[O-])C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323442 86925 0 None -4 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 348 4 0 7 1.9 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)c3ccccc3[N+](=O)[O-])C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL308924 103760 0 None 2 2 Human 4.4 pKi = 4.4 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 268 4 1 5 1.0 CCO/C(O)=C1\CN2CC(CCC2CN(C)C)C1=O 10.1021/jm020572p
155552185 174037 0 None -67608 16 Human 4.4 pKi = 4.4 Binding
Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 174037 0 None -67608 16 Human 4.4 pKi = 4.4 Binding
Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)Displacement of [3H] NMS from muscarinic M3 receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
25067048 12301 0 None -29 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 646 13 2 2 8.1 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1185245 12301 0 None -29 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 646 13 2 2 8.1 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL402207 12301 0 None -29 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 646 13 2 2 8.1 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCC(C2CC[N+](C)(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
21509921 104431 0 None -371 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104431 0 None -371 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
28417 40009 49 None -1 12 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL1479 40009 49 None -1 12 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
191 402 98 None -37 29 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 402 98 None -37 29 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 402 98 None -37 29 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 402 98 None -37 29 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 402 98 None -37 29 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
3198 205490 76 None -10 34 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205490 76 None -10 34 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205490 76 None -10 34 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
43815 186896 64 None -5 25 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
CHEMBL1708 186896 64 None -5 25 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
CHEMBL490 186896 64 None -5 25 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
90666113 109318 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 744 18 6 9 7.5 Cc1cc(C)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c(-c2ccc(O)c(Cl)c2)c1 10.1039/C1MD00140J
CHEMBL3219045 109318 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 744 18 6 9 7.5 Cc1cc(C)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c(-c2ccc(O)c(Cl)c2)c1 10.1039/C1MD00140J
132947 3835 9 None -309 9 Human 7.4 pKi = 7.4 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/s0960-894x(01)00186-x
361 3835 9 None -309 9 Human 7.4 pKi = 7.4 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/s0960-894x(01)00186-x
CHEMBL265256 3835 9 None -309 9 Human 7.4 pKi = 7.4 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1016/s0960-894x(01)00186-x
155519740 170382 0 None -141 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 3 hrs by beta counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 3 hrs by beta counting method
ChEMBL 1125 29 4 14 9.6 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCNCC(=O)N1c2ncccc2NC(=O)c2cccnc21 10.1021/acs.jmedchem.8b01967
CHEMBL4448108 170382 0 None -141 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 3 hrs by beta counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 3 hrs by beta counting method
ChEMBL 1125 29 4 14 9.6 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CCCCCCNCC(=O)N1c2ncccc2NC(=O)c2cccnc21 10.1021/acs.jmedchem.8b01967
21509921 104431 0 None -371 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104431 0 None -371 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M3 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
422063 196054 2 None -2 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 298 6 0 2 3.1 C[N+](C)(C)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2377384 196054 2 None -2 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 298 6 0 2 3.1 C[N+](C)(C)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL560649 196054 2 None -2 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 298 6 0 2 3.1 C[N+](C)(C)CCOC(=O)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
44593619 187436 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493980 187436 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
44400180 68979 0 None 1 2 Rat 7.4 pKi = 7.4 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 397 5 1 4 2.7 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2005.02.036
CHEMBL192337 68979 0 None 1 2 Rat 7.4 pKi = 7.4 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 397 5 1 4 2.7 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2005.02.036
44379281 57516 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 506 9 1 5 5.3 CCOC(=O)N(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/S0960-894X(97)00109-1
CHEMBL166385 57516 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 506 9 1 5 5.3 CCOC(=O)N(CC)CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/S0960-894X(97)00109-1
86720830 192136 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 490 8 2 7 3.6 Cn1nc(C(=O)O)cc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
CHEMBL5203937 192136 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 490 8 2 7 3.6 Cn1nc(C(=O)O)cc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
70683405 74446 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2021477 74446 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2027984 74446 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
155511112 169503 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 394 7 0 4 4.4 COc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4435123 169503 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 394 7 0 4 4.4 COc1ccc(CCCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1 10.1016/j.bmcl.2018.12.022
137630994 161116 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 234 3 0 1 2.5 COc1cccc2c1CC(C[N+](C)(C)C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4103375 161116 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 234 3 0 1 2.5 COc1cccc2c1CC(C[N+](C)(C)C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4117267 161116 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 234 3 0 1 2.5 COc1cccc2c1CC(C[N+](C)(C)C)CC2 10.1021/acs.jmedchem.7b01113
448537 160226 89 None -28 25 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 160226 89 None -28 25 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
44437295 11861 0 None -4 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 222 2 0 4 1.2 C(#CCN1CCCCC1)COC1=NOCC1 10.1016/j.bmc.2007.09.003
CHEMBL1182472 11861 0 None -4 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 222 2 0 4 1.2 C(#CCN1CCCCC1)COC1=NOCC1 10.1016/j.bmc.2007.09.003
CHEMBL239866 11861 0 None -4 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 222 2 0 4 1.2 C(#CCN1CCCCC1)COC1=NOCC1 10.1016/j.bmc.2007.09.003
10262466 98316 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 208 2 0 3 0.3 O=C1CCON1CC#CCN1CCCC1 10.1016/j.bmc.2007.09.003
CHEMBL275104 98316 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 208 2 0 3 0.3 O=C1CCON1CC#CCN1CCCC1 10.1016/j.bmc.2007.09.003
44409769 76503 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 4 3.6 C[C@@H]1C[C@H]1c1nc(NC2CC2)cc(N2CCCCCC2)n1 10.1016/j.bmcl.2006.01.006
CHEMBL206087 76503 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 286 4 1 4 3.6 C[C@@H]1C[C@H]1c1nc(NC2CC2)cc(N2CCCCCC2)n1 10.1016/j.bmcl.2006.01.006
44409796 76727 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 5 2 4 4.4 Cc1c(NC2CCCCCC2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
CHEMBL206780 76727 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 5 2 4 4.4 Cc1c(NC2CCCCCC2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
44409965 76947 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 306 5 1 6 2.5 COc1c(NC2CC2)nc(C2CC2)nc1N1CCSCC1 10.1016/j.bmcl.2006.01.006
CHEMBL207098 76947 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 306 5 1 6 2.5 COc1c(NC2CC2)nc(C2CC2)nc1N1CCSCC1 10.1016/j.bmcl.2006.01.006
10030021 169855 12 None -50 5 Human 6.4 pKi = 6.4 Binding
Binding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 532 10 1 4 6.1 CCCC(C)(C)C(=O)N(CC)CCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4440484 169855 12 None -50 5 Human 6.4 pKi = 6.4 Binding
Binding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cellsBinding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 532 10 1 4 6.1 CCCC(C)(C)C(=O)N(CC)CCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
145961495 161422 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@]1(C(=O)O[C@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4127373 161422 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@]1(C(=O)O[C@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
10982070 5134 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 392 2 0 6 3.7 COC(=O)c1c(C)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL105945 5134 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 392 2 0 6 3.7 COC(=O)c1c(C)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
10486393 141677 0 None -436 5 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL1202000 141677 0 None -436 5 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
CHEMBL385625 141677 0 None -436 5 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CC(=O)N1c2ccccc2NC(=O)c2cccnc21)CCCCCCNCC(=O)N1c2ccccc2NC(=O)c2cccnc21 10.1021/jm981038d
24809738 11857 0 None -79 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 209 3 0 3 1.1 Cc1cc(OCC#CC[N+](C)(C)C)no1 10.1016/j.bmc.2007.09.003
CHEMBL1182466 11857 0 None -79 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 209 3 0 3 1.1 Cc1cc(OCC#CC[N+](C)(C)C)no1 10.1016/j.bmc.2007.09.003
CHEMBL239655 11857 0 None -79 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 209 3 0 3 1.1 Cc1cc(OCC#CC[N+](C)(C)C)no1 10.1016/j.bmc.2007.09.003
15157138 99597 0 None -1 4 Human 8.4 pKi = 8.4 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 345 9 0 3 4.8 CCN(CC)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL284137 99597 0 None -1 4 Human 8.4 pKi = 8.4 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 345 9 0 3 4.8 CCN(CC)CCCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
44406406 133512 0 None 12 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 340 3 1 4 2.6 COC1(C#CC(O)(c2ccccn2)C2CCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL370862 133512 0 None 12 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 340 3 1 4 2.6 COC1(C#CC(O)(c2ccccn2)C2CCCC2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
59291452 112749 0 None 1 3 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.1 O=C(Nc1ccsc1-c1ccccc1)O[C@@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298590 112749 0 None 1 3 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.1 O=C(Nc1ccsc1-c1ccccc1)O[C@@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305615 112749 0 None 1 3 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 328 3 1 4 4.1 O=C(Nc1ccsc1-c1ccccc1)O[C@@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
71452754 79508 0 None -1 2 Rat 8.4 pKi = 8.4 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00090a006
CHEMBL2114061 79508 0 None -1 2 Rat 8.4 pKi = 8.4 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1[C@@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00090a006
44420821 84259 0 None 15 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 437 5 1 2 5.2 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CC2CCC(C1)N2Cc1ccccc1 10.1021/jm061159a
CHEMBL221400 84259 0 None 15 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 437 5 1 2 5.2 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CC2CCC(C1)N2Cc1ccccc1 10.1021/jm061159a
2286 3161 51 None -1 30 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3161 51 None -1 30 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3161 51 None -1 30 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3161 51 None -1 30 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3161 51 None -1 30 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
44593625 188106 0 None -1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL498358 188106 0 None -1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL539120 188106 0 None -1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
9821459 200420 11 None 4 3 Human 8.4 pKi = 8.4 Binding
Binding affinity for human cloned Muscarinic M3 receptorsBinding affinity for human cloned Muscarinic M3 receptors
ChEMBL 384 7 2 3 4.0 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(99)00327-3
CHEMBL59836 200420 11 None 4 3 Human 8.4 pKi = 8.4 Binding
Binding affinity for human cloned Muscarinic M3 receptorsBinding affinity for human cloned Muscarinic M3 receptors
ChEMBL 384 7 2 3 4.0 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1016/s0960-894x(99)00327-3
44431391 146396 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 352 6 1 5 2.3 CN(C)C1(CNCCC2CCOCC2)COc2ccc(F)cc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL392186 146396 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 352 6 1 5 2.3 CN(C)C1(CNCCC2CCOCC2)COc2ccc(F)cc2OC1 10.1016/j.bmcl.2006.11.058
16086003 80402 0 None 114 4 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 608 9 3 5 3.5 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL214642 80402 0 None 114 4 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 608 9 3 5 3.5 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
9821459 200420 11 None 4 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 384 7 2 3 4.0 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1021/jm0003135
CHEMBL59836 200420 11 None 4 3 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 384 7 2 3 4.0 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)C2CCCC2)CC1 10.1021/jm0003135
4134 72657 12 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 342 8 1 3 3.0 CC[N+](C)(CC)CCOC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL1996652 72657 12 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 342 8 1 3 3.0 CC[N+](C)(CC)CCOC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2106570 72657 12 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 342 8 1 3 3.0 CC[N+](C)(CC)CCOC(=O)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
15108133 111274 0 None -3 2 Rat 8.4 pKi = 8.4 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 335 4 0 3 3.8 CN1CC2CC1C[C@@H](OC(=O)C(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL326640 111274 0 None -3 2 Rat 8.4 pKi = 8.4 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 335 4 0 3 3.8 CN1CC2CC1C[C@@H](OC(=O)C(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
90666119 109326 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 728 19 6 9 6.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@H]3C[C@@]3(COC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
CHEMBL3219052 109326 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 728 19 6 9 6.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@H]3C[C@@]3(COC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
CHEMBL5274390 193789 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 366 3 2 3 4.6 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OC1CCNCC1 10.1021/acs.jmedchem.2c01376
16125680 136612 0 None 70 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 429 5 1 2 4.8 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(F)c2)CC1 10.1021/jm061159a
CHEMBL373994 136612 0 None 70 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 429 5 1 2 4.8 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(F)c2)CC1 10.1021/jm061159a
90666114 109320 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3cc(F)ccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219047 109320 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3cc(F)ccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
90666117 109324 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 744 20 6 9 7.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219050 109324 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 744 20 6 9 7.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
16125683 84621 0 None 36 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 431 5 1 2 5.5 Cc1cccc(CN2CCC(N3CC(c4ccccc4)(C4CCCCC4)NC3=O)CC2)c1 10.1021/jm061159a
CHEMBL222403 84621 0 None 36 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 431 5 1 2 5.5 Cc1cccc(CN2CCC(N3CC(c4ccccc4)(C4CCCCC4)NC3=O)CC2)c1 10.1021/jm061159a
53326837 58515 0 None 7 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 722 17 5 10 5.3 C[N+]1(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)[C@@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@H]12 10.1016/j.bmcl.2011.01.043
CHEMBL1683942 58515 0 None 7 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 722 17 5 10 5.3 C[N+]1(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)[C@@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@H]12 10.1016/j.bmcl.2011.01.043
118719921 115748 0 None 1 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 115748 0 None 1 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
54580133 61786 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 654 19 5 7 7.7 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773265 61786 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 654 19 5 7 7.7 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
140844405 176618 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 9 1 3 5.1 O=C(OC1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4474694 176618 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 9 1 3 5.1 O=C(OC1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597973 176618 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 470 9 1 3 5.1 O=C(OC1C[N+]2(CCCCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
90666111 109316 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 730 18 6 9 7.2 Cc1ccc(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c(-c2ccc(O)c(Cl)c2)c1 10.1039/C1MD00140J
CHEMBL3219043 109316 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 730 18 6 9 7.2 Cc1ccc(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c(-c2ccc(O)c(Cl)c2)c1 10.1039/C1MD00140J
53322411 58487 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 380 8 1 3 5.9 CCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683914 58487 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 380 8 1 3 5.9 CCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
16125682 84260 0 None 239 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 465 5 1 2 5.0 O=C1NC(c2ccc(F)cc2)(c2ccc(F)cc2)CN1C1CCN(Cc2cccc(F)c2)CC1 10.1021/jm061159a
CHEMBL221401 84260 0 None 239 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 465 5 1 2 5.0 O=C1NC(c2ccc(F)cc2)(c2ccc(F)cc2)CN1C1CCN(Cc2cccc(F)c2)CC1 10.1021/jm061159a
16115943 11815 0 None -5 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL1182205 11815 0 None -5 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
CHEMBL220393 11815 0 None -5 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1 10.1021/jm061374r
44431380 87956 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 318 5 1 4 2.9 CN(C)C1(CNCC2CCCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL234257 87956 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 318 5 1 4 2.9 CN(C)C1(CNCC2CCCCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
44406346 136125 0 None 6 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 361 4 1 3 3.2 COC1(C#CC(O)(Cc2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL373256 136125 0 None 6 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 361 4 1 3 3.2 COC1(C#CC(O)(Cc2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
6075 150084 42 None -3 16 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 150084 42 None -3 16 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
44430470 86776 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 316 4 0 5 2.9 COC1CN(c2nc(C3CC3)nc(N3CCCCCC3)c2C)C1 10.1016/j.bmcl.2007.03.047
CHEMBL232208 86776 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 316 4 0 5 2.9 COC1CN(c2nc(C3CC3)nc(N3CCCCCC3)c2C)C1 10.1016/j.bmcl.2007.03.047
44430457 150646 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 328 3 0 4 4.4 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2007.03.047
CHEMBL395571 150646 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 328 3 0 4 4.4 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2007.03.047
44409981 76207 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2CC2)nc(C2CCC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205840 76207 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2CC2)nc(C2CCC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
70681307 74427 0 None -9 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2021479 74427 0 None -9 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2027890 74427 0 None -9 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
137630891 161105 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 2 0 1 2.3 COc1cccc2c1CCC([N+](C)(C)C)C2 10.1021/acs.jmedchem.7b01113
CHEMBL4085451 161105 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 2 0 1 2.3 COc1cccc2c1CCC([N+](C)(C)C)C2 10.1021/acs.jmedchem.7b01113
CHEMBL4117201 161105 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 2 0 1 2.3 COc1cccc2c1CCC([N+](C)(C)C)C2 10.1021/acs.jmedchem.7b01113
44437256 12364 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 282 4 0 4 2.8 C(#CCN1CCCC1)COc1cc(-c2ccccc2)on1 10.1016/j.bmc.2007.09.003
CHEMBL1185707 12364 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 282 4 0 4 2.8 C(#CCN1CCCC1)COc1cc(-c2ccccc2)on1 10.1016/j.bmc.2007.09.003
CHEMBL428916 12364 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 282 4 0 4 2.8 C(#CCN1CCCC1)COc1cc(-c2ccccc2)on1 10.1016/j.bmc.2007.09.003
15050946 102619 0 None -1 4 Rat 5.4 pKi = 5.4 Binding
Compound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to mmuscarinic acetylcholine receptor M3 of transfected rat A9L cellsCompound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to mmuscarinic acetylcholine receptor M3 of transfected rat A9L cells
ChEMBL 484 5 2 6 2.5 CNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
CHEMBL304391 102619 0 None -1 4 Rat 5.4 pKi = 5.4 Binding
Compound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to mmuscarinic acetylcholine receptor M3 of transfected rat A9L cellsCompound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to mmuscarinic acetylcholine receptor M3 of transfected rat A9L cells
ChEMBL 484 5 2 6 2.5 CNC(=O)c1ccc(CN2CCN(CC(=O)N3c4ccccc4C(=O)Nc4cccnc43)CC2)cc1 10.1021/jm00111a032
15730 71089 80 None -1 10 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
CHEMBL195437 71089 80 None -1 10 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1 nan
122194377 123983 0 None 1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 412 8 1 5 3.6 COc1ccc(CCNC(=O)OCC2(c3ccccc3)CCN(C)CC2)cc1OC 10.1016/j.bmcl.2015.10.029
CHEMBL3629536 123983 0 None 1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 412 8 1 5 3.6 COc1ccc(CCNC(=O)OCC2(c3ccccc3)CCN(C)CC2)cc1OC 10.1016/j.bmcl.2015.10.029
71452382 83765 0 None -12 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205812 83765 0 None -12 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1 10.1016/j.bmcl.2012.08.046
11079969 163833 0 None -26 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 404 4 1 5 4.3 C=CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL420662 163833 0 None -26 5 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 404 4 1 5 4.3 C=CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
71575027 86194 0 None -8 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 379 8 0 4 4.4 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccc(OC)cc2)C1 10.1021/jm301774u
CHEMBL2312389 86194 0 None -8 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 379 8 0 4 4.4 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccc(OC)cc2)C1 10.1021/jm301774u
10066369 120232 0 None -67 6 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL352375 120232 0 None -67 6 Human 5.4 pKi = 5.4 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 348 7 0 2 5.7 CC(C1=C(CCN(C(C)C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
44448538 12387 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 339 6 1 2 3.1 C[N+]1(C)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1185855 12387 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 339 6 1 2 3.1 C[N+]1(C)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL436850 12387 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 339 6 1 2 3.1 C[N+]1(C)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
44274400 98910 0 None -1 5 Human 4.4 pKi = 4.4 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL279520 98910 0 None -1 5 Human 4.4 pKi = 4.4 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
46227487 14095 0 None 1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 216 2 0 2 1.7 CC1(C)OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198047 14095 0 None 1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 216 2 0 2 1.7 CC1(C)OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL593861 14095 0 None 1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 216 2 0 2 1.7 CC1(C)OC[C@@H](C[N+](C)(C)C)OC1(C)C 10.1016/j.bmc.2009.10.027
137630667 161068 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 204 3 0 1 2.7 C[N+](C)(C)CCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
CHEMBL4100938 161068 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 204 3 0 1 2.7 C[N+](C)(C)CCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116890 161068 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 204 3 0 1 2.7 C[N+](C)(C)CCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
140844418 176386 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 10 1 4 4.9 O=C(OC1C[N+]2(CCCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4576060 176386 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 10 1 4 4.9 O=C(OC1C[N+]2(CCCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596067 176386 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 10 1 4 4.9 O=C(OC1C[N+]2(CCCCOc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
75356563 156933 23 None 1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 184 3 1 4 1.0 c1csc(COC2CCNC2)n1 10.1021/acs.jmedchem.7b01113
CHEMBL4072787 156933 23 None 1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 184 3 1 4 1.0 c1csc(COC2CCNC2)n1 10.1021/acs.jmedchem.7b01113
631645 164852 1 None -1 3 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 565 9 3 8 2.4 CC(C)(C)OC(=O)NCCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL422053 164852 1 None -1 3 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 565 9 3 8 2.4 CC(C)(C)OC(=O)NCCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
44593622 187772 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL495888 187772 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL556390 187772 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
145960427 161426 0 None -3 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@@]1(C(=O)O[C@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL4127428 161426 0 None -3 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 407 4 0 5 3.4 C[C@@]1(C(=O)O[C@H]2CN3CCC2CC3)COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
16125623 138099 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 436 5 1 3 4.5 N#Cc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
CHEMBL376636 138099 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 436 5 1 3 4.5 N#Cc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
10026270 94086 0 None 18 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 440 6 2 3 4.5 O=C(N[C@H]1[C@@H]2CN(Cc3ccc4ccccc4c3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL249206 94086 0 None 18 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 440 6 2 3 4.5 O=C(N[C@H]1[C@@H]2CN(Cc3ccc4ccccc4c3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
140844397 176574 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 10 1 4 4.7 O=C(OC1C[N+]2(CCCOCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4567385 176574 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 10 1 4 4.7 O=C(OC1C[N+]2(CCCOCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597612 176574 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 10 1 4 4.7 O=C(OC1C[N+]2(CCCOCc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
44593618 187435 0 None -4 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493979 187435 0 None -4 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
155528419 171304 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 6 0 4 4.0 COc1ccc(CCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4461216 171304 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 6 0 4 4.0 COc1ccc(CCOC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1 10.1016/j.bmcl.2018.12.022
137639541 156679 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 3 0 3 1.7 CN1CCCC(OCc2cccnc2)C1 10.1021/acs.jmedchem.7b01113
CHEMBL4070061 156679 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 3 0 3 1.7 CN1CCCC(OCc2cccnc2)C1 10.1021/acs.jmedchem.7b01113
10963509 18464 1 None -48 5 Human 6.4 pKi = 6.4 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 687 17 0 6 8.6 COc1ccccc1CN1CCC(C2CCN(CCCCCCCCN3CCC(C4CCN(Cc5ccccc5OC)CC4)CC3)CC2)CC1 10.1021/jm0155594
CHEMBL127273 18464 1 None -48 5 Human 6.4 pKi = 6.4 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 687 17 0 6 8.6 COc1ccccc1CN1CCC(C2CCN(CCCCCCCCN3CCC(C4CCN(Cc5ccccc5OC)CC4)CC3)CC2)CC1 10.1021/jm0155594
71454526 79430 0 None 1 2 Rat 5.4 pKi = 5.4 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@@H]1C[C@@H]2C[C@H](C1)N([C@H](C)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL2113669 79430 0 None 1 2 Rat 5.4 pKi = 5.4 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 273 3 0 3 3.2 CC(=O)O[C@@H]1C[C@@H]2C[C@H](C1)N([C@H](C)c1ccccc1)C2 10.1021/jm00115a003
10344314 94084 0 None 12 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 462 8 2 5 3.1 COC(=O)c1ccc(CCN2C[C@H]3[C@H](NC(=O)C(O)(c4ccccc4)C4CCCC4)[C@H]3C2)cc1 10.1016/j.bmcl.2007.06.081
CHEMBL249204 94084 0 None 12 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 462 8 2 5 3.1 COC(=O)c1ccc(CCN2C[C@H]3[C@H](NC(=O)C(O)(c4ccccc4)C4CCCC4)[C@H]3C2)cc1 10.1016/j.bmcl.2007.06.081
10365534 154936 0 None 18 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 432 7 2 3 4.0 Cc1ccc(CCN2C[C@H]3[C@H](NC(=O)C(O)(c4ccccc4)C4CCCC4)[C@H]3C2)cc1C 10.1016/j.bmcl.2007.06.081
CHEMBL401154 154936 0 None 18 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 432 7 2 3 4.0 Cc1ccc(CCN2C[C@H]3[C@H](NC(=O)C(O)(c4ccccc4)C4CCCC4)[C@H]3C2)cc1C 10.1016/j.bmcl.2007.06.081
156015971 178258 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4648444 178258 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650880 178258 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 318 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@](c2ccccc2)(C2CCCCC2)CO1 10.1021/acs.jmedchem.9b02100
145961161 161582 0 None -4 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@H](CO[C@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
CHEMBL4129580 161582 0 None -4 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@H](CO[C@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
10092649 193049 56 None -38 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1021/jm100697g
CHEMBL522460 193049 56 None -38 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1021/jm100697g
2230 464 60 None -588 10 Human 4.4 pKi = 4.4 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
296 464 60 None -588 10 Human 4.4 pKi = 4.4 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
CHEMBL7303 464 60 None -588 10 Human 4.4 pKi = 4.4 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
DB04365 464 60 None -588 10 Human 4.4 pKi = 4.4 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm020572p
137628858 160947 0 None -1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 5 0 1 2.3 CCOc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4074319 160947 0 None -1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 5 0 1 2.3 CCOc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115967 160947 0 None -1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 5 0 1 2.3 CCOc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
155510347 174687 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 398 7 0 5 4.0 COc1ccc(CCN(C(=O)OC2CCCN(C)C2)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4559952 174687 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 398 7 0 5 4.0 COc1ccc(CCN(C(=O)OC2CCCN(C)C2)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
2551 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
298 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
488 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
CHEMBL965 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
DB00411 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0510878
162353388 180955 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC[C@H]1CO 10.1016/j.bmcl.2020.127632
CHEMBL4758633 180955 0 None -8 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC[C@H]1CO 10.1016/j.bmcl.2020.127632
44448457 11881 0 None -3 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 566 15 2 2 6.6 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1182638 11881 0 None -3 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 566 15 2 2 6.6 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL257586 11881 0 None -3 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 566 15 2 2 6.6 C[N+](C)(CCCC(O)(c1ccccc1)c1ccccc1)CC[N+](C)(C)CCCC(O)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
2551 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
298 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
488 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
CHEMBL965 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
DB00411 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
2551 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
298 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
488 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
CHEMBL965 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
DB00411 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm800145d
7022778 172759 11 None 1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc([C@@H]2CCCN2)c1 10.1021/jm800145d
CHEMBL451335 172759 11 None 1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 137 1 1 2 1.7 c1coc([C@@H]2CCCN2)c1 10.1021/jm800145d
2551 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
298 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
488 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
CHEMBL965 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
DB00411 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2009.10.027
2551 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
298 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
488 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
CHEMBL965 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
DB00411 791 23 None -346 11 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2014.06.020
1548953 207656 27 None -2 17 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 207656 27 None -2 17 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
2726 916 68 None -18 73 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 916 68 None -18 73 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 916 68 None -18 73 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 916 68 None -18 73 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 916 68 None -18 73 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
155556290 176432 0 None -257 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4554682 176432 0 None -257 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596434 176432 0 None -257 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 923 22 7 11 3.1 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
70687661 74424 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2021476 74424 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
CHEMBL2027845 74424 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(C)[C@@H]1CCCC[C@H]1N(C)CC(=O)N1c2ccccc2NC(=O)c2ccccc21 10.1016/j.bmc.2008.06.025
118719924 115752 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 649 20 0 7 8.4 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354071 115752 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 649 20 0 7 8.4 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
11610557 72002 0 None -8 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1CC(O)c2ccccc2C1c1ccccc1 10.1021/jm050099q
CHEMBL197588 72002 0 None -8 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 378 2 1 4 3.4 O=C(O[C@H]1CN2CCC1CC2)N1CC(O)c2ccccc2C1c1ccccc1 10.1021/jm050099q
15050935 203947 0 None -1 2 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 381 3 2 6 1.1 CN1CCN(CC(=O)N2c3cc(CO)ccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL69423 203947 0 None -1 2 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 381 3 2 6 1.1 CN1CCN(CC(=O)N2c3cc(CO)ccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
156014875 178217 0 None -3 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4640846 178217 0 None -3 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650577 178217 0 None -3 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
162657652 180961 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 335 4 1 3 4.2 CCn1c2ccccc2c2ccc(NCC(=O)N3CCCCC3)cc21 10.1016/j.bmcl.2020.127632
CHEMBL4758742 180961 0 None -1 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 335 4 1 3 4.2 CCn1c2ccccc2c2ccc(NCC(=O)N3CCCCC3)cc21 10.1016/j.bmcl.2020.127632
24894631 176740 3 None -1 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCCC1c1ccco1 10.1021/jm800145d
CHEMBL460470 176740 3 None -1 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCCC1c1ccco1 10.1021/jm800145d
46227411 14089 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
CHEMBL1198027 14089 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
CHEMBL593443 14089 0 None -2 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
2551 791 23 None -54 11 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44318736 106994 0 None -3 4 Human 6.4 pKi = 6.4 Binding
The binding affinity was measured as inhibition of binding of [3H]- quinuclidinyl benzilate to m3 Muscarinic acetylcholine receptor M3 in membranes of CHO cellsThe binding affinity was measured as inhibition of binding of [3H]- quinuclidinyl benzilate to m3 Muscarinic acetylcholine receptor M3 in membranes of CHO cells
ChEMBL 276 3 1 5 2.0 O=C(OC1CC2CCCC1N2)c1ccc([N+](=O)[O-])cc1 10.1021/jm9904001
CHEMBL315428 106994 0 None -3 4 Human 6.4 pKi = 6.4 Binding
The binding affinity was measured as inhibition of binding of [3H]- quinuclidinyl benzilate to m3 Muscarinic acetylcholine receptor M3 in membranes of CHO cellsThe binding affinity was measured as inhibition of binding of [3H]- quinuclidinyl benzilate to m3 Muscarinic acetylcholine receptor M3 in membranes of CHO cells
ChEMBL 276 3 1 5 2.0 O=C(OC1CC2CCCC1N2)c1ccc([N+](=O)[O-])cc1 10.1021/jm9904001
19716 9235 6 None - 1 Rat 5.4 pKi = 5.4 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 194 2 0 2 0.6 CC(=O)N(C)CC#CCN1CCCC1 10.1021/jm00164a044
CHEMBL11081 9235 6 None - 1 Rat 5.4 pKi = 5.4 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 194 2 0 2 0.6 CC(=O)N(C)CC#CCN1CCCC1 10.1021/jm00164a044
10114698 4801 0 None -41 5 Human 6.3 pKi = 6.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 448 7 1 5 5.5 CCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL104210 4801 0 None -41 5 Human 6.3 pKi = 6.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 448 7 1 5 5.5 CCCCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
133640439 181349 1 None -7 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 1.9 O=C(O)C1CCCN1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
CHEMBL4763304 181349 1 None -7 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 1.9 O=C(O)C1CCCN1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
44274433 99482 0 None -2 5 Human 4.3 pKi = 4.3 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL283320 99482 0 None -2 5 Human 4.3 pKi = 4.3 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2ccncc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
10851461 58481 42 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 296 3 2 3 3.7 O=C(Nc1ccccc1-c1ccccc1)OC1CCNCC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683908 58481 42 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 296 3 2 3 3.7 O=C(Nc1ccccc1-c1ccccc1)OC1CCNCC1 10.1016/j.bmcl.2011.01.043
15050953 102312 0 None -2 4 Rat 7.3 pKi = 7.3 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 536 9 2 7 4.0 CC(C)(C)OC(=O)NCCCCCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL303684 102312 0 None -2 4 Rat 7.3 pKi = 7.3 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 536 9 2 7 4.0 CC(C)(C)OC(=O)NCCCCCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
9985181 120332 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 556 9 1 4 6.1 CCN(CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1)C(=O)c1ccc(F)cc1 10.1016/S0960-894X(97)00109-1
CHEMBL353140 120332 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 556 9 1 4 6.1 CCN(CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1)C(=O)c1ccc(F)cc1 10.1016/S0960-894X(97)00109-1
122194373 123981 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 397 8 0 5 3.8 COc1ccc(CCC(=O)OCC2(c3ccccc3)CCN(C)CC2)cc1OC 10.1016/j.bmcl.2015.10.029
CHEMBL3629533 123981 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 397 8 0 5 3.8 COc1ccc(CCC(=O)OCC2(c3ccccc3)CCN(C)CC2)cc1OC 10.1016/j.bmcl.2015.10.029
2551 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
73355415 92504 0 None -2 13 Human 6.3 pKi = 6.3 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
CHEMBL2432039 92504 0 None -2 13 Human 6.3 pKi = 6.3 Binding
Inhibition of muscarinic M3 receptor (unknown origin) by PDSP assayInhibition of muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
44593617 187407 0 None -3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL493795 187407 0 None -3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
14939893 9502 0 None -112 5 Rat 6.3 pKi = 6.3 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 621 24 3 7 6.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL112244 9502 0 None -112 5 Rat 6.3 pKi = 6.3 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 621 24 3 7 6.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
44337638 110539 0 None -1 2 Rat 4.3 pKi = 4.3 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
CHEMBL325322 110539 0 None -1 2 Rat 4.3 pKi = 4.3 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
137642607 158494 0 None -2398 8 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 348 5 0 2 4.2 O=C1CCc2ccccc2N1CCCN1CCC(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4091231 158494 0 None -2398 8 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 348 5 0 2 4.2 O=C1CCc2ccccc2N1CCCN1CCC(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
156016047 178236 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4647816 178236 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
CHEMBL4650722 178236 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 312 4 0 2 3.6 C[N+](C)(C)C[C@@H]1CO[C@@H](c2ccccc2)[C@H](c2ccccc2)O1 10.1021/acs.jmedchem.9b02100
46227481 14107 0 None 1 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL1198081 14107 0 None 1 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
CHEMBL595022 14107 0 None 1 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 202 2 0 2 1.3 C[C@H]1O[C@H](C[N+](C)(C)C)COC1(C)C 10.1016/j.bmc.2009.10.027
1530 2169 50 None -57 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2169 50 None -57 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2169 50 None -57 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2169 50 None -57 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2169 50 None -57 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
2551 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44309151 203560 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 380 6 2 3 3.3 NCCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL66820 203560 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 380 6 2 3 3.3 NCCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
2200 3109 46 None -7 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
328 3109 46 None -7 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
4848 3109 46 None -7 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
CHEMBL9967 3109 46 None -7 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
DB00670 3109 46 None -7 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1016/j.bmc.2008.06.025
187 255 39 None -26 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 255 39 None -26 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 255 39 None -26 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 255 39 None -26 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 255 39 None -26 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 255 39 None -26 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
137629744 161151 0 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1ccccc1CC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL4071109 161151 0 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1ccccc1CC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL4117602 161151 0 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1ccccc1CC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
44437298 11855 0 None -21 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 237 2 0 3 1.4 C[N+]1(CC#CCOC2=NOCC2)CCCCC1 10.1016/j.bmc.2007.09.003
CHEMBL1182460 11855 0 None -21 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 237 2 0 3 1.4 C[N+]1(CC#CCOC2=NOCC2)CCCCC1 10.1016/j.bmc.2007.09.003
CHEMBL239436 11855 0 None -21 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 237 2 0 3 1.4 C[N+]1(CC#CCOC2=NOCC2)CCCCC1 10.1016/j.bmc.2007.09.003
71452791 79622 0 None -21 2 Rat 4.3 pKi = 4.3 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 245 3 0 3 2.2 CC(=O)O[C@@H]1CC2CC1N(Cc1ccccc1)C2 10.1021/jm00090a006
CHEMBL2115123 79622 0 None -21 2 Rat 4.3 pKi = 4.3 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 245 3 0 3 2.2 CC(=O)O[C@@H]1CC2CC1N(Cc1ccccc1)C2 10.1021/jm00090a006
3652 46214 70 None -1 9 Human 5.3 pKi = 5.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 10.1038/s41586-020-2286-9
CHEMBL1535 46214 70 None -1 9 Human 5.3 pKi = 5.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 10.1038/s41586-020-2286-9
53325043 58492 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 450 13 1 3 7.9 CCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683919 58492 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 450 13 1 3 7.9 CCCCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
16086039 12308 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 2 4 4.8 N[C@H]1CCCC[C@@H]1NC(=O)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL1185290 12308 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 2 4 4.8 N[C@H]1CCCC[C@@H]1NC(=O)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL405117 12308 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 8 2 4 4.8 N[C@H]1CCCC[C@@H]1NC(=O)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
155550632 176505 0 None -776 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 845 22 8 10 1.9 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4540949 176505 0 None -776 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 845 22 8 10 1.9 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4597071 176505 0 None -776 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 845 22 8 10 1.9 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
70685504 74425 0 None -14 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)[C@H]1CCCC[C@H]1N(C)C 10.1016/j.bmc.2008.06.025
CHEMBL2021478 74425 0 None -14 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)[C@H]1CCCC[C@H]1N(C)C 10.1016/j.bmc.2008.06.025
CHEMBL2027846 74425 0 None -14 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 406 4 1 4 3.7 CN(CC(=O)N1c2ccccc2NC(=O)c2ccccc21)[C@H]1CCCC[C@H]1N(C)C 10.1016/j.bmc.2008.06.025
23352285 96750 2 None -4 3 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 219 2 0 3 2.6 O=Cc1ccc(C2=CN3CCC2CC3)s1 10.1016/S0960-894X(01)80824-6
CHEMBL264747 96750 2 None -4 3 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 219 2 0 3 2.6 O=Cc1ccc(C2=CN3CCC2CC3)s1 10.1016/S0960-894X(01)80824-6
71575652 86169 0 None -9 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 381 5 0 4 3.6 CN1CCC(c2ccccc2F)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
CHEMBL2312352 86169 0 None -9 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 381 5 0 4 3.6 CN1CCC(c2ccccc2F)=C(C(=O)OCCc2ccc3c(c2)CCO3)C1 10.1021/jm301774u
11759058 120823 0 None -1 5 Human 4.3 pKi = 4.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL355851 120823 0 None -1 5 Human 4.3 pKi = 4.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 321 6 1 3 2.3 CN(C)CCNC(=O)C1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
11674313 65957 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 329 3 1 4 3.4 Fc1cccc(F)c1-n1nc(OC2CCNCC2)c2ccccc21 10.1021/jm2007535
CHEMBL1836644 65957 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylscopolamine from human M3 receptorDisplacement of [3H]N-methylscopolamine from human M3 receptor
ChEMBL 329 3 1 4 3.4 Fc1cccc(F)c1-n1nc(OC2CCNCC2)c2ccccc21 10.1021/jm2007535
16086017 12270 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL1184940 12270 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL379483 12270 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NCC1CCNCC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
6098192 201778 14 None -1 3 Rat 6.3 pKi = 6.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@@H]1CN2CCC1CC2)N1CCc2ccccc2[C@H]1c1ccccc1 10.1021/jm050099q
CHEMBL606901 201778 14 None -1 3 Rat 6.3 pKi = 6.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@@H]1CN2CCC1CC2)N1CCc2ccccc2[C@H]1c1ccccc1 10.1021/jm050099q
2551 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44337748 9363 0 None 1 2 Rat 5.3 pKi = 5.3 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
CHEMBL111529 9363 0 None 1 2 Rat 5.3 pKi = 5.3 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
59707195 109313 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(F)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219040 109313 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(F)c3)CC2)ccc1O 10.1039/C1MD00140J
16115801 12263 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL1184882 12263 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL375851 12263 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 340 3 0 2 4.3 C[N+]1(C)CCC[C@@H]1[C@@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
72712474 106426 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 310 3 1 5 1.1 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3091669 106426 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 310 3 1 5 1.1 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
CHEMBL3139993 106426 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assayBinding affinity to wild type human M3 receptor expressed in HEK293T cells up to 24 hrs by radioligand displacement assay
ChEMBL 310 3 1 5 1.1 C[N+]1(C)[C@H]2C[C@@H](OC(=O)C(O)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1021/jm401219y
9809330 115973 0 None -45 5 Human 8.3 pKi = 8.3 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0301235
CHEMBL335542 115973 0 None -45 5 Human 8.3 pKi = 8.3 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0301235
168289650 191476 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 504 8 2 5 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)cc2F)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5193776 191476 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 504 8 2 5 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)cc2F)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
15888010 203823 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 3 2 3 2.3 NC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL68584 203823 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 338 3 2 3 2.3 NC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
53321086 58488 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 394 9 1 3 6.3 CCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683915 58488 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 394 9 1 3 6.3 CCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
16115950 136357 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
CHEMBL373515 136357 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned muscarinic receptor M3 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M3 expressed in CHO cells
ChEMBL 325 3 0 3 4.1 CN1CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1 10.1021/jm061374r
2028 2958 80 None -1 11 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm050099q
359 2958 80 None -1 11 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm050099q
4634 2958 80 None -1 11 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm050099q
CHEMBL1231 2958 80 None -1 11 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm050099q
DB01062 2958 80 None -1 11 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1021/jm050099q
10470 2471 7 None -11 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
1689 2471 7 None -11 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
4057 2471 7 None -11 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
CHEMBL524004 2471 7 None -11 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
DB04843 2471 7 None -11 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 10.1016/j.bmc.2019.06.016
44404147 169066 12 None -3 3 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1c1ccccc1 10.1021/jm050099q
CHEMBL439867 169066 12 None -3 3 Rat 8.3 pKi = 8.3 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 362 2 0 3 3.9 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1c1ccccc1 10.1021/jm050099q
10646948 37852 0 None -4 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 444 6 3 4 3.8 O=C(NC1CCN(Cc2cccc(O)c2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
CHEMBL145913 37852 0 None -4 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 444 6 3 4 3.8 O=C(NC1CCN(Cc2cccc(O)c2)CC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1021/jm0003135
180 400 56 None -23 40 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 400 56 None -23 40 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 400 56 None -23 40 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 400 56 None -23 40 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 400 56 None -23 40 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
5648 78382 9 None -1 5 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
CHEMBL2107687 78382 9 None -1 5 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
CHEMBL2111176 78382 9 None -1 5 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 nan
44431388 87290 0 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 348 6 1 5 2.8 CN(C)C1(CNCCC2=CCSCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL233202 87290 0 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 348 6 1 5 2.8 CN(C)C1(CNCCC2=CCSCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
9883040 100509 0 None -14 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human muscarinic M3 receptorBinding affinity towards human muscarinic M3 receptor
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL291339 100509 0 None -14 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human muscarinic M3 receptorBinding affinity towards human muscarinic M3 receptor
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL542622 100509 0 None -14 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human muscarinic M3 receptorBinding affinity towards human muscarinic M3 receptor
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
10025038 168803 0 None 26 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 6 2 3 4.3 CC(c1ccccc1)N1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
CHEMBL437781 168803 0 None 26 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 6 2 3 4.3 CC(c1ccccc1)N1C[C@H]2[C@H](NC(=O)C(O)(c3ccccc3)C3CCCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
11796509 40667 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 422 7 2 4 3.9 COc1cccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)c1 10.1021/jm0003135
CHEMBL148450 40667 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 422 7 2 4 3.9 COc1cccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)c1 10.1021/jm0003135
2381 660 48 None -9 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
374 660 48 None -9 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
7128 660 48 None -9 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
CHEMBL1101 660 48 None -9 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
DB00810 660 48 None -9 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1016/j.bmc.2013.01.072
73345823 89786 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 305 10 0 3 4.1 CC[C@H](C)C(C(=O)OCCCN(CC)CC)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL2377392 89786 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 305 10 0 3 4.1 CC[C@H](C)C(C(=O)OCCCN(CC)CC)c1ccccc1 10.1016/j.bmc.2013.01.072
44400175 67739 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 307 5 1 2 4.2 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@H]3C2)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
CHEMBL190815 67739 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 307 5 1 2 4.2 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@H]3C2)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
44308910 203719 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 324 3 2 3 1.7 O=C(N1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL67814 203719 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 324 3 2 3 1.7 O=C(N1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
44406527 140624 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 349 3 1 5 1.8 CO[C@]1(C#CC(O)(c2cccnc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL381469 140624 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 349 3 1 5 1.8 CO[C@]1(C#CC(O)(c2cccnc2)c2cccnc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
53319786 58494 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 339 5 2 4 3.3 NCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683920 58494 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 339 5 2 4 3.3 NCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
155536739 172191 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 384 5 0 4 4.1 COc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
CHEMBL4473985 172191 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 384 5 0 4 4.1 COc1ccc(COC(=O)N(c2ccccc2)C2CN3CCC2CC3)cc1F 10.1016/j.bmcl.2018.12.022
44409651 76363 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 5 1 4 3.9 CCC1CCN(c2nc(C3CC3)nc(NC3CC3)c2C)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL205944 76363 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 5 1 4 3.9 CCC1CCN(c2nc(C3CC3)nc(NC3CC3)c2C)CC1 10.1016/j.bmcl.2006.01.006
10171570 77028 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 272 2 1 4 3.1 C1CCCN(c2nc(C3CC3)nc3c2CCCN3)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL207287 77028 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 272 2 1 4 3.1 C1CCCN(c2nc(C3CC3)nc3c2CCCN3)CC1 10.1016/j.bmcl.2006.01.006
44409463 140690 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 308 4 1 4 3.5 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(F)(F)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL381752 140690 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 308 4 1 4 3.5 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(F)(F)CC1 10.1016/j.bmcl.2006.01.006
10619926 39772 0 None 2 3 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 382 6 2 4 3.4 O=C(NC1CCN(Cc2ccoc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL147672 39772 0 None 2 3 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 382 6 2 4 3.4 O=C(NC1CCN(Cc2ccoc2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
10316726 11996 0 None -40 5 Rat 7.3 pKi = 7.3 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
CHEMBL1183364 11996 0 None -40 5 Rat 7.3 pKi = 7.3 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
CHEMBL292857 11996 0 None -40 5 Rat 7.3 pKi = 7.3 Binding
Compound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary GlandCompound was tested for inhibiting [3H]N-Methyl-scopolamine Binding to Muscarinic receptor (M3) in Rat Submaxillary Gland
ChEMBL 364 2 0 3 3.6 C[N+]1(C)C2CCC1CC1(C2)OC(=O)C(c2ccccc2)(c2ccccc2)O1 10.1016/0960-894X(95)00403-G
16094783 136542 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL373888 136542 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
10951142 5190 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 496 6 0 6 5.9 CCOC(=O)c1c(CC)n(Cc2ccccc2)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL106219 5190 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 496 6 0 6 5.9 CCOC(=O)c1c(CC)n(Cc2ccccc2)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
44430474 86975 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 290 3 0 4 2.9 FC1CN(c2cc(N3CCCCCC3)nc(C3CC3)n2)C1 10.1016/j.bmcl.2007.03.047
CHEMBL232417 86975 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 290 3 0 4 2.9 FC1CN(c2cc(N3CCCCCC3)nc(C3CC3)n2)C1 10.1016/j.bmcl.2007.03.047
44409461 74746 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 302 5 2 5 2.4 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(CO)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL203124 74746 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 302 5 2 5 2.4 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(CO)CC1 10.1016/j.bmcl.2006.01.006
44409556 75992 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 288 4 2 5 2.2 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(O)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL205582 75992 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 288 4 2 5 2.2 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(O)CC1 10.1016/j.bmcl.2006.01.006
44409963 77287 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 336 5 1 4 4.3 Cc1c(NC2CC2)nc(Cc2ccccc2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL208300 77287 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 336 5 1 4 4.3 Cc1c(NC2CC2)nc(Cc2ccccc2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
10925451 58742 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2ccc(Cl)cc21)c1ccccn1 10.1021/jm020895l
CHEMBL168707 58742 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2ccc(Cl)cc21)c1ccccn1 10.1021/jm020895l
11120347 120703 0 None 1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 Cc1ccc2c(c1)CC(CCN(C)C)=C2C(C)c1ccccn1 10.1021/jm020895l
CHEMBL354841 120703 0 None 1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 Cc1ccc2c(c1)CC(CCN(C)C)=C2C(C)c1ccccn1 10.1021/jm020895l
137655636 158712 0 None -234 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 376 7 0 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4093527 158712 0 None -234 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 376 7 0 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
44299635 100541 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](C#C[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL291562 100541 0 None -4 4 Human 5.3 pKi = 5.3 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 343 0 0 3 3.9 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](C#C[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
155543345 176662 0 None -537 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4543584 176662 0 None -537 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4598362 176662 0 None -537 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
6604789 101020 5 None -199 10 Human 4.3 pKi = 4.3 Binding
Binding affinity against Muscarinic M3 receptorBinding affinity against Muscarinic M3 receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
CHEMBL294649 101020 5 None -199 10 Human 4.3 pKi = 4.3 Binding
Binding affinity against Muscarinic M3 receptorBinding affinity against Muscarinic M3 receptor
ChEMBL 311 3 1 4 1.6 Cn1cc(C(=O)C(=O)N[C@H]2CN3CCC2CC3)c2ccccc21 10.1016/0960-894X(95)00308-G
16125533 84627 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 400 7 1 1 4.2 C[N+](C)(CCN1CC(c2ccccc2)(c2ccccc2)NC1=O)Cc1ccccc1 10.1021/jm061160+
CHEMBL222426 84627 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 400 7 1 1 4.2 C[N+](C)(CCN1CC(c2ccccc2)(c2ccccc2)NC1=O)Cc1ccccc1 10.1021/jm061160+
44593623 187856 0 None -4 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496503 187856 0 None -4 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL539373 187856 0 None -4 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 356 3 0 2 3.3 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
2551 791 23 None -346 11 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
298 791 23 None -346 11 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
488 791 23 None -346 11 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL965 791 23 None -346 11 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB00411 791 23 None -346 11 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
56963799 74866 0 None -1288 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to human recombinant M3 receptorBinding affinity to human recombinant M3 receptor
ChEMBL 378 6 0 5 4.6 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1 10.1021/jm201690h
CHEMBL2031737 74866 0 None -1288 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to human recombinant M3 receptorBinding affinity to human recombinant M3 receptor
ChEMBL 378 6 0 5 4.6 C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1 10.1021/jm201690h
44627958 14004 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197374 14004 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569089 14004 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
44593616 193190 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
CHEMBL523518 193190 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 341 3 0 3 3.1 CN1CCC[C@@H]1[C@@H]1C[S+]([O-])C(c2ccccc2)(c2ccccc2)O1 10.1016/j.bmc.2008.04.013
10916286 5070 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(Cl)c2C1O3 10.1021/jm011116o
CHEMBL105593 5070 0 None -2 4 Human 5.3 pKi = 5.3 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 396 2 1 4 4.8 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(Cl)c2C1O3 10.1021/jm011116o
137645406 157878 0 None -64 13 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4084262 157878 0 None -64 13 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 491 8 0 7 5.4 COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1 10.1021/acs.jmedchem.9b00412
3055 1421 44 None -1 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
313 1421 44 None -1 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
7163 1421 44 None -1 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
CHEMBL936 1421 44 None -1 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
DB01231 1421 44 None -1 9 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 nan
14537188 136521 0 None -16 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 341 8 1 4 3.6 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccc(O)cc1 10.1016/j.bmc.2013.01.072
CHEMBL37372 136521 0 None -16 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 341 8 1 4 3.6 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccc(O)cc1 10.1016/j.bmc.2013.01.072
9978073 94039 0 None 7 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 396 6 2 4 3.4 O=C(N[C@H]1[C@@H]2CN(Cc3cccs3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL249005 94039 0 None 7 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 396 6 2 4 3.4 O=C(N[C@H]1[C@@H]2CN(Cc3cccs3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
154734599 2486 12 None -19 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
327 2486 12 None -19 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
4108 2486 12 None -19 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
CHEMBL27673 2486 12 None -19 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cellsDisplacement of [3H] N-methyl-scopolamine chloride from human muscarinic receptor M3 expressed in CHO cells
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmc.2007.01.022
162353390 180925 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 2.1 O=C(CCN1CCCc2ccccc21)N1CCCC(CO)C1 10.1016/j.bmcl.2020.127632
CHEMBL4758316 180925 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 302 4 1 3 2.1 O=C(CCN1CCCc2ccccc21)N1CCCC(CO)C1 10.1016/j.bmcl.2020.127632
44448385 11878 0 None -4 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 406 7 1 3 4.8 CN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182633 11878 0 None -4 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 406 7 1 3 4.8 CN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL257174 11878 0 None -4 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 406 7 1 3 4.8 CN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.03.061
162353377 181141 0 None -14 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 2 0 2 2.8 CC1CCc2ccccc2N1CC(=O)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4760904 181141 0 None -14 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 2 0 2 2.8 CC1CCc2ccccc2N1CC(=O)N1CCCCC1 10.1016/j.bmcl.2020.127632
24894514 172710 3 None -1 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@H]1c1ccco1 10.1021/jm800145d
CHEMBL450729 172710 3 None -1 5 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@H]1c1ccco1 10.1021/jm800145d
122194369 123977 0 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 383 7 0 5 3.5 COc1ccc(CCOC(=O)C2(c3ccccc3)CCN(C)CC2)cc1OC 10.1016/j.bmcl.2015.10.029
CHEMBL3629529 123977 0 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 383 7 0 5 3.5 COc1ccc(CCOC(=O)C2(c3ccccc3)CCN(C)CC2)cc1OC 10.1016/j.bmcl.2015.10.029
16125679 84990 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 479 5 1 2 5.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(C(F)(F)F)c2)CC1 10.1021/jm061159a
CHEMBL223925 84990 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 479 5 1 2 5.6 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(C(F)(F)F)c2)CC1 10.1021/jm061159a
44437270 12296 0 None -13 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 222 2 0 3 0.6 O=C1CCON1CC#CCN1CCCCC1 10.1016/j.bmc.2007.09.003
CHEMBL1185211 12296 0 None -13 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 222 2 0 3 0.6 O=C1CCON1CC#CCN1CCCCC1 10.1016/j.bmc.2007.09.003
CHEMBL398043 12296 0 None -13 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 222 2 0 3 0.6 O=C1CCON1CC#CCN1CCCCC1 10.1016/j.bmc.2007.09.003
155551903 176433 0 None -67 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 462 8 2 4 4.3 CCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4569929 176433 0 None -67 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 462 8 2 4 4.3 CCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596435 176433 0 None -67 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 462 8 2 4 4.3 CCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
162353378 182887 0 None -8 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC(O)C1 10.1016/j.bmcl.2020.127632
CHEMBL4792360 182887 0 None -8 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC(O)C1 10.1016/j.bmcl.2020.127632
16125593 84712 0 None 2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 467 8 1 3 4.1 N#CC[N+]1(CCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222916 84712 0 None 2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 467 8 1 3 4.1 N#CC[N+]1(CCOc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
2551 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
71450550 83778 0 None -1 16 Human 6.3 pKi = 6.3 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205836 83778 0 None -1 16 Human 6.3 pKi = 6.3 Binding
Binding affinity to M3 muscarinic receptorBinding affinity to M3 muscarinic receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
1210 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
1213 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
2725 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
33036 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
4411 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
616 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
6976 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
716121 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
90475904 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 915 51 None -79 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
155528270 176367 0 None -457 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4461081 176367 0 None -457 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595943 176367 0 None -457 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
44448500 12302 0 None -4 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 549 12 2 3 6.2 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1185248 12302 0 None -4 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 549 12 2 3 6.2 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL402282 12302 0 None -4 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 549 12 2 3 6.2 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
162658421 181077 0 None -11 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 3 0 2 3.6 CC1CCCC(C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
CHEMBL4760150 181077 0 None -11 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 3 0 2 3.6 CC1CCCC(C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
53326338 58483 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 324 4 1 3 4.4 CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683910 58483 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 324 4 1 3 4.4 CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
10104167 2046 2 None -60 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 10.1021/acs.jmedchem.7b01113
6937 2046 2 None -60 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL3121473 2046 2 None -60 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 10.1021/acs.jmedchem.7b01113
155516845 170085 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 364 6 0 3 4.4 O=C(OCCCc1ccccc1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4443613 170085 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 364 6 0 3 4.4 O=C(OCCCc1ccccc1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
2551 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44437303 12294 1 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 271 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc21 10.1016/j.bmc.2007.09.003
CHEMBL1185162 12294 1 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 271 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc21 10.1016/j.bmc.2007.09.003
CHEMBL394329 12294 1 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 271 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc21 10.1016/j.bmc.2007.09.003
44431372 87286 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 368 7 1 4 3.7 CC(C)c1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 10.1016/j.bmcl.2006.11.058
CHEMBL233198 87286 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 368 7 1 4 3.7 CC(C)c1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 10.1016/j.bmcl.2006.11.058
26987 946 33 None -56 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
6063 946 33 None -56 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
671 946 33 None -56 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
CHEMBL1626 946 33 None -56 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
DB00283 946 33 None -56 21 Human 7.3 pKi = 7.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41586-020-2286-9
118719931 115759 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 669 18 0 4 8.7 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)CC1 10.1021/jm501173q
CHEMBL3354078 115759 0 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 669 18 0 4 8.7 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)CC1 10.1021/jm501173q
155525691 171007 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CCN(C)CC2)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4456775 171007 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 368 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CCN(C)CC2)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
2230 464 60 None -1348 10 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
296 464 60 None -1348 10 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
CHEMBL7303 464 60 None -1348 10 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
DB04365 464 60 None -1348 10 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
2230 464 60 None -588 10 Human 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
296 464 60 None -588 10 Human 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
CHEMBL7303 464 60 None -588 10 Human 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
DB04365 464 60 None -588 10 Human 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm9705115
10957754 59014 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 6 0 2 4.5 CC(C1=C(CCCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL169401 59014 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 6 0 2 4.5 CC(C1=C(CCCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
118719929 115757 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 442 15 1 3 6.0 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354076 115757 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 442 15 1 3 6.0 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCCCO)CC1 10.1021/jm501173q
10606253 157249 0 None -2290 5 Rat 5.2 pKi = 5.2 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1152 27 4 13 9.2 CN(CCCCCCCCN(C)C(=O)CCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
CHEMBL407678 157249 0 None -2290 5 Rat 5.2 pKi = 5.2 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 1152 27 4 13 9.2 CN(CCCCCCCCN(C)C(=O)CCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm981038d
71454562 79625 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 436 6 0 4 5.5 COc1ccc([S@+]([O-])c2ccc(C(C#N)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL2115126 79625 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 436 6 0 4 5.5 COc1ccc([S@+]([O-])c2ccc(C(C#N)C3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
10251468 94040 0 None 20 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 6 2 3 4.2 Cc1ccc(C(C)N2C[C@H]3[C@H](NC(=O)C(O)(c4ccccc4)C4CCCC4)[C@H]3C2)cc1 10.1016/j.bmcl.2007.06.081
CHEMBL249006 94040 0 None 20 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 6 2 3 4.2 Cc1ccc(C(C)N2C[C@H]3[C@H](NC(=O)C(O)(c4ccccc4)C4CCCC4)[C@H]3C2)cc1 10.1016/j.bmcl.2007.06.081
55005 104748 8 None -14 3 Rat 6.2 pKi = 6.2 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 208 2 0 2 1.0 CC(=O)N(C)C(C)C#CCN1CCCC1 10.1021/jm00164a044
CHEMBL310852 104748 8 None -14 3 Rat 6.2 pKi = 6.2 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 208 2 0 2 1.0 CC(=O)N(C)C(C)C#CCN1CCCC1 10.1021/jm00164a044
137630084 161021 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 1 0 1 1.8 COc1cccc2c1C[N+](C)(C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4070055 161021 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 1 0 1 1.8 COc1cccc2c1C[N+](C)(C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116507 161021 0 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 192 1 0 1 1.8 COc1cccc2c1C[N+](C)(C)CC2 10.1021/acs.jmedchem.7b01113
137629673 161135 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 198 3 0 0 2.6 C[N+](C)(C)CCc1cccc(Cl)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4094819 161135 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 198 3 0 0 2.6 C[N+](C)(C)CCc1cccc(Cl)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4117396 161135 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 198 3 0 0 2.6 C[N+](C)(C)CCc1cccc(Cl)c1 10.1021/acs.jmedchem.7b01113
425249 89768 8 None -10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 355 8 1 4 3.6 CC(C)N(CCOC(=O)C(O)(c1ccccc1)c1ccccc1)C(C)C 10.1016/j.bmc.2013.01.072
CHEMBL2377261 89768 8 None -10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 355 8 1 4 3.6 CC(C)N(CCOC(=O)C(O)(c1ccccc1)c1ccccc1)C(C)C 10.1016/j.bmc.2013.01.072
155563428 175262 0 None -79 5 Human 5.2 pKi = 5.2 Binding
Inhibition of muscarinic M3 receptor (unknown origin)Inhibition of muscarinic M3 receptor (unknown origin)
ChEMBL 475 7 3 9 2.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
CHEMBL4572905 175262 0 None -79 5 Human 5.2 pKi = 5.2 Binding
Inhibition of muscarinic M3 receptor (unknown origin)Inhibition of muscarinic M3 receptor (unknown origin)
ChEMBL 475 7 3 9 2.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b01662
2551 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
9998202 69137 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Ki value for rat Muscarinic acetylcholine receptor M3Ki value for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
CHEMBL192485 69137 0 None 2 2 Rat 8.2 pKi = 8.2 Binding
Ki value for rat Muscarinic acetylcholine receptor M3Ki value for rat Muscarinic acetylcholine receptor M3
ChEMBL 353 5 1 4 2.6 O=C(OCC#CCN1CC2CC2C1)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2005.02.036
54586985 61783 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 583 15 5 7 5.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773262 61783 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assayDisplacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
ChEMBL 583 15 5 7 5.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
10647703 120942 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 461 6 3 4 3.8 Nc1ccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)cc1F 10.1021/jm0003135
CHEMBL356181 120942 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 461 6 3 4 3.8 Nc1ccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)cc1F 10.1021/jm0003135
10622033 42752 0 None 3 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 420 7 2 3 4.2 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1021/jm0003135
CHEMBL150219 42752 0 None 3 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 420 7 2 3 4.2 CC(C)=CCCN1CCC(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1021/jm0003135
CHEMBL5273907 193761 0 None -7 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 945 20 2 5 13.3 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCCCCN3CCC(COC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
10193093 76423 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 298 4 1 4 3.5 Cc1c(NC2CC2)nc(C2CC2)nc1N1CC2CCC(C2)C1 10.1016/j.bmcl.2006.01.006
CHEMBL205976 76423 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 298 4 1 4 3.5 Cc1c(NC2CC2)nc(C2CC2)nc1N1CC2CCC(C2)C1 10.1016/j.bmcl.2006.01.006
CHEMBL5078006 214505 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
168291613 192010 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 476 8 2 6 4.5 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cc(C(=O)O)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5202045 192010 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 476 8 2 6 4.5 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cc(C(=O)O)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
118737353 119033 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 705 13 6 9 5.2 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426700 119033 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 705 13 6 9 5.2 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
16065136 67897 0 None 3 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2ccccc2)C1 10.1021/jm200884j
CHEMBL1910847 67897 0 None 3 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cells after 2 hrs by filter binding assay
ChEMBL 442 9 1 3 5.2 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC[C@@H](Oc2ccccc2)C1 10.1021/jm200884j
10525412 41944 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 406 6 2 3 4.2 Cc1ccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)cc1 10.1021/jm0003135
CHEMBL149486 41944 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 406 6 2 3 4.2 Cc1ccc(CN2CCC(NC(=O)C(O)(c3ccccc3)C3CCCC3)CC2)cc1 10.1021/jm0003135
11968014 12726 5 None -5 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/jm301774u
CHEMBL1187846 12726 5 None -5 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cellsDisplacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells
ChEMBL 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 10.1021/jm301774u
140844422 176417 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 490 8 1 3 5.4 O=C(OC1C[N+]2(CCCc3cccc(Cl)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4452706 176417 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 490 8 1 3 5.4 O=C(OC1C[N+]2(CCCc3cccc(Cl)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4596309 176417 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 490 8 1 3 5.4 O=C(OC1C[N+]2(CCCc3cccc(Cl)c3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
24846938 89772 0 None -5 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 339 8 1 5 3.4 CCN(CC)CCOC(=O)C(O)(c1cccs1)C1CCCCC1 10.1016/j.bmc.2013.01.072
CHEMBL2377267 89772 0 None -5 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 339 8 1 5 3.4 CCN(CC)CCOC(=O)C(O)(c1cccs1)C1CCCCC1 10.1016/j.bmc.2013.01.072
16124705 84600 0 None 77 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 451 5 1 2 5.8 O=C1NC(c2ccccc2)(C2CCCCC2)CN1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm061159a
CHEMBL222207 84600 0 None 77 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 451 5 1 2 5.8 O=C1NC(c2ccccc2)(C2CCCCC2)CN1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm061159a
138711334 177302 0 None 3 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 382 4 2 3 4.5 O=C(Nc1ccc(F)cc1-c1cc(F)c(F)c(F)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4637155 177302 0 None 3 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 382 4 2 3 4.5 O=C(Nc1ccc(F)cc1-c1cc(F)c(F)c(F)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
16125335 138133 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 454 6 1 2 4.3 C[N+]1(C[C@H]2O[C@@H]2c2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL376900 138133 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 454 6 1 2 4.3 C[N+]1(C[C@H]2O[C@@H]2c2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
11595794 135676 0 None -2 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 3 4.4 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1C1CCCCC1 10.1021/jm050099q
CHEMBL372983 135676 0 None -2 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 3 4.4 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1C1CCCCC1 10.1021/jm050099q
16125681 84739 0 None 141 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 481 5 1 2 5.6 O=C1NC(c2ccc(F)cc2)(c2ccc(F)cc2)CN1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm061159a
CHEMBL223079 84739 0 None 141 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 481 5 1 2 5.6 O=C1NC(c2ccc(F)cc2)(c2ccc(F)cc2)CN1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm061159a
16125585 84723 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 456 8 1 2 4.4 C[N+]1(CCOCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222976 84723 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 456 8 1 2 4.4 C[N+]1(CCOCc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
10204457 204380 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 453 6 0 6 4.0 COc1ccc(S(=O)(=O)c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
CHEMBL71971 204380 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Binding affinity against Muscarinic acetylcholine receptor M3Binding affinity against Muscarinic acetylcholine receptor M3
ChEMBL 453 6 0 6 4.0 COc1ccc(S(=O)(=O)c2ccc(C(C#N)N3CCN(C4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(00)00437-6
44431387 87289 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 350 6 1 5 2.9 CN(C)C1(CNCCC2CCSCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL233201 87289 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
ChEMBL 350 6 1 5 2.9 CN(C)C1(CNCCC2CCSCC2)COc2ccccc2OC1 10.1016/j.bmcl.2006.11.058
CHEMBL5283759 194205 0 None -2 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1024 19 1 13 9.4 CN(C)c1ccc2c(-c3ccc(-c4cn(CCCCCn5cc(CCCCCN6CCC(OC(=O)Nc7ccc(F)cc7-c7ccc(F)c(Cl)c7)CC6)nn5)nn4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1021/acs.jmedchem.2c01376
44443724 93960 0 None 51 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 6 2 3 4.1 O=C(N[C@H]1[C@@H]2CN(Cc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL248614 93960 0 None 51 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 6 2 3 4.1 O=C(N[C@H]1[C@@H]2CN(Cc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCCCC1 10.1016/j.bmcl.2007.06.081
10670917 165040 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 443 6 3 4 3.7 Nc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
CHEMBL422665 165040 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 443 6 3 4 3.7 Nc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)c1 10.1021/jm0003135
5387 94850 31 None -4 6 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O 10.1021/jm00111a032
CHEMBL253978 94850 31 None -4 6 Rat 8.2 pKi = 8.2 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O 10.1021/jm00111a032
44593626 187829 0 None -1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL496306 187829 0 None -1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL539121 187829 0 None -1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@@H]1[C@@H]1C[S+]([O-])[C@@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
155511167 169534 0 None 2 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 432 6 0 3 5.7 O=C(OCCCc1ccc(Cl)c(Cl)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4435641 169534 0 None 2 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 432 6 0 3 5.7 O=C(OCCCc1ccc(Cl)c(Cl)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
155565770 175600 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 410 7 0 5 4.0 COc1ccc(CCN(C(=O)OC2CN3CCC2CC3)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
CHEMBL4580590 175600 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 410 7 0 5 4.0 COc1ccc(CCN(C(=O)OC2CN3CCC2CC3)c2ccccc2)cc1OC 10.1016/j.bmcl.2018.12.022
162353380 182470 0 None -1 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 259 2 0 3 1.8 O=C(CN1CCCc2cnccc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4786868 182470 0 None -1 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 259 2 0 3 1.8 O=C(CN1CCCc2cnccc21)N1CCCCC1 10.1016/j.bmcl.2020.127632
155560305 176229 0 None -257 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 801 19 5 9 2.8 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4568151 176229 0 None -257 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 801 19 5 9 2.8 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4594890 176229 0 None -257 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 801 19 5 9 2.8 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.8b01967
57326233 77157 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042406 77157 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079010 77157 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 312 4 0 2 3.1 C[N+](C)(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
16125470 84626 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 426 5 1 1 4.8 C[N+]1(Cc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061160+
CHEMBL222425 84626 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 426 5 1 1 4.8 C[N+]1(Cc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061160+
145963288 161591 0 None -3 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@@H](CO[C@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
CHEMBL4129723 161591 0 None -3 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 379 5 0 4 3.5 c1ccc(C2(c3ccccc3)COC[C@@H](CO[C@H]3CN4CCC3CC4)O2)cc1 10.1016/j.ejmech.2017.06.004
300 2493 15 None -3 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 10.1021/jm800145d
4141 2493 15 None -3 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 10.1021/jm800145d
CHEMBL92387 2493 15 None -3 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 10.1021/jm800145d
44274317 83343 0 None -2 5 Human 4.2 pKi = 4.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21937 83343 0 None -2 5 Human 4.2 pKi = 4.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 319 5 1 3 2.7 CN(C)CCNC(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
44446841 12306 0 None -2 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1185281 12306 0 None -2 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL404557 12306 0 None -2 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
101176697 168853 25 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 1963 53 22 24 -4.3 CC(=O)NC(C)(C)C(=O)N1CCC[C@H]1C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@H](C(=O)NC(C)(C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NC(C)(C)C(=O)NC(C)(C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CO)Cc1ccccc1)C(C)C)C(C)C 10.1021/jm061160+
16132042 168853 25 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 1963 53 22 24 -4.3 CC(=O)NC(C)(C)C(=O)N1CCC[C@H]1C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@H](C(=O)NC(C)(C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NC(C)(C)C(=O)NC(C)(C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CO)Cc1ccccc1)C(C)C)C(C)C 10.1021/jm061160+
CHEMBL438243 168853 25 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 1963 53 22 24 -4.3 CC(=O)NC(C)(C)C(=O)N1CCC[C@H]1C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@H](C(=O)NC(C)(C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NC(C)(C)C(=O)NC(C)(C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CO)Cc1ccccc1)C(C)C)C(C)C 10.1021/jm061160+
631644 204054 1 None -1 3 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 551 8 3 8 2.0 CC(C)(C)OC(=O)NCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL70133 204054 1 None -1 3 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 551 8 3 8 2.0 CC(C)(C)OC(=O)NCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
137631178 161180 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 5 0 1 2.3 COc1cccc(CCC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4081662 161180 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 5 0 1 2.3 COc1cccc(CCC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4117768 161180 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 208 5 0 1 2.3 COc1cccc(CCC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
2551 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
11595794 135676 0 None -2 3 Rat 7.2 pKi = 7.2 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 3 4.4 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1C1CCCCC1 10.1021/jm050099q
CHEMBL372983 135676 0 None -2 3 Rat 7.2 pKi = 7.2 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
ChEMBL 368 2 0 3 4.4 O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2C1C1CCCCC1 10.1021/jm050099q
44406572 72813 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 347 3 1 3 3.0 CO[C@@]1(C#CC(O)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL200208 72813 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 347 3 1 3 3.0 CO[C@@]1(C#CC(O)(c2ccccc2)c2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44409745 140099 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 272 4 1 4 3.3 c1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL380135 140099 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 272 4 1 4 3.3 c1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
44409976 140448 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 330 6 2 4 4.1 Cc1c(NCc2c(F)cccc2F)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
CHEMBL380954 140448 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 330 6 2 4 4.1 Cc1c(NCc2c(F)cccc2F)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
122203596 155782 0 None -50 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 627 14 3 7 4.3 CCC(=O)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1016/j.ejmech.2021.113159
CHEMBL4059733 155782 0 None -50 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 627 14 3 7 4.3 CCC(=O)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1016/j.ejmech.2021.113159
CHEMBL4066481 155782 0 None -50 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 627 14 3 7 4.3 CCC(=O)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1016/j.ejmech.2021.113159
129989 450 51 None -16 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
8584 450 51 None -16 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
CHEMBL43383 450 51 None -16 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 10.1021/acs.jmedchem.8b01967
162649253 183621 0 None -57 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 807 12 1 6 7.9 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
CHEMBL4748004 183621 0 None -57 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 807 12 1 6 7.9 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
CHEMBL4802611 183621 0 None -57 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 807 12 1 6 7.9 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCN1CCN(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1039/d0md00137f
25025581 201973 0 None 1 8 Human 7.2 pKi = 7.2 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 285 4 1 2 3.1 CCOC[C@H]1[C@@H]2CNC[C@@]21c1ccc(Cl)c(Cl)c1 10.1021/jm901818u
CHEMBL608151 201973 0 None 1 8 Human 7.2 pKi = 7.2 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 285 4 1 2 3.1 CCOC[C@H]1[C@@H]2CNC[C@@]21c1ccc(Cl)c(Cl)c1 10.1021/jm901818u
1016 3720 78 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3720 78 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3720 78 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3720 78 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3720 78 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3720 78 None -12 35 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
11045444 59159 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 7 0 2 4.9 CCCC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL170088 59159 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 7 0 2 4.9 CCCC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
156009698 178312 0 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 872 16 2 5 11.0 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4634575 178312 0 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 872 16 2 5 11.0 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651200 178312 0 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 872 16 2 5 11.0 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
118719927 115755 0 None -6 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354074 115755 0 None -6 8 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
71459909 78586 0 None 3 2 Human 6.2 pKi = 6.2 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 444 5 0 3 6.4 O=C(c1cccs1)N(c1c(Cl)cccc1Cl)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL2112313 78586 0 None 3 2 Human 6.2 pKi = 6.2 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 444 5 0 3 6.4 O=C(c1cccs1)N(c1c(Cl)cccc1Cl)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
137629935 160996 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4060823 160996 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116342 160996 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
2551 791 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
298 791 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
488 791 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
CHEMBL965 791 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
DB00411 791 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
155522355 176385 0 None -5011 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4451030 176385 0 None -5011 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4596065 176385 0 None -5011 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1016/j.ejmech.2021.113159
2551 791 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 791 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 791 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 791 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 791 23 None -346 11 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
44274417 98866 0 None -6 5 Human 4.2 pKi = 4.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 333 5 0 3 3.0 CN(C)CCN(C)C(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL279225 98866 0 None -6 5 Human 4.2 pKi = 4.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 333 5 0 3 3.0 CN(C)CCN(C)C(=O)C1=C/C(=C\c2ccccn2)c2ccccc21 10.1016/s0960-894x(01)00186-x
44339221 8693 0 None - 1 Rat 4.2 pKi = 4.2 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heartThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heart
ChEMBL 220 2 0 3 2.0 CCC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
CHEMBL109593 8693 0 None - 1 Rat 4.2 pKi = 4.2 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heartThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heart
ChEMBL 220 2 0 3 2.0 CCC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
44406342 72141 0 None 5 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 375 5 1 3 3.3 COC1(C#CC(O)(Cc2ccccc2)Cc2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL197973 72141 0 None 5 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 375 5 1 3 3.3 COC1(C#CC(O)(Cc2ccccc2)Cc2ccccc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44430469 168684 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 300 3 0 5 2.4 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(=O)C1 10.1016/j.bmcl.2007.03.047
CHEMBL436814 168684 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 300 3 0 5 2.4 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(=O)C1 10.1016/j.bmcl.2007.03.047
24962988 182588 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 324 5 1 3 3.7 CCOC(=O)N(Cc1ccccc1-c1ccccc1)[C@H]1CCNC1 10.1016/j.bmcl.2008.06.071
CHEMBL478834 182588 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 324 5 1 3 3.7 CCOC(=O)N(Cc1ccccc1-c1ccccc1)[C@H]1CCNC1 10.1016/j.bmcl.2008.06.071
122194370 123979 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 353 6 0 4 3.4 COc1ccc(CCOC(=O)C2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
CHEMBL3629530 123979 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysisDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells after 2 hrs by liquid scintillation spectrometry analysis
ChEMBL 353 6 0 4 3.4 COc1ccc(CCOC(=O)C2(c3ccccc3)CCN(C)CC2)cc1 10.1016/j.bmcl.2015.10.029
132947 3835 9 None -999 9 Rat 6.2 pKi = 6.2 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00075a032
361 3835 9 None -999 9 Rat 6.2 pKi = 6.2 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00075a032
CHEMBL265256 3835 9 None -999 9 Rat 6.2 pKi = 6.2 Binding
Affinity constant measured against M3 muscarinic receptor in rat submaxillary glandAffinity constant measured against M3 muscarinic receptor in rat submaxillary gland
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00075a032
164617895 188501 0 None -3467 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 24 10 13 -0.5 CC(=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)N[C@H](CCCN)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4852868 188501 0 None -3467 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 24 10 13 -0.5 CC(=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)N[C@H](CCCN)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028466 188501 0 None -3467 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 931 24 10 13 -0.5 CC(=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)N[C@H](CCCN)C(=O)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
155560013 176276 0 None -154 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4564922 176276 0 None -154 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595198 176276 0 None -154 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
132947 3835 9 None -999 9 Rat 6.2 pKi = 6.2 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00046a021
361 3835 9 None -999 9 Rat 6.2 pKi = 6.2 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00046a021
CHEMBL265256 3835 9 None -999 9 Rat 6.2 pKi = 6.2 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 10.1021/jm00046a021
44309107 102148 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 360 5 3 3 3.4 NCc1ccc(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)cc1 10.1016/s0960-894x(03)00350-0
CHEMBL302720 102148 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 360 5 3 3 3.4 NCc1ccc(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)cc1 10.1016/s0960-894x(03)00350-0
2551 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
24841480 183875 0 None -33 20 Human 7.2 pKi = 7.2 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 183875 0 None -33 20 Human 7.2 pKi = 7.2 Binding
Antagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M3 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
119357 303 49 None -16 6 Human 7.2 pKi = 7.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1016/s0960-894x(01)00186-x
3264 303 49 None -16 6 Human 7.2 pKi = 7.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1016/s0960-894x(01)00186-x
368 303 49 None -16 6 Human 7.2 pKi = 7.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1016/s0960-894x(01)00186-x
CHEMBL279453 303 49 None -16 6 Human 7.2 pKi = 7.2 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1016/s0960-894x(01)00186-x
119357 303 49 None -16 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1021/acs.jmedchem.8b01967
3264 303 49 None -16 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1021/acs.jmedchem.8b01967
368 303 49 None -16 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1021/acs.jmedchem.8b01967
CHEMBL279453 303 49 None -16 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay
ChEMBL 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 10.1021/acs.jmedchem.8b01967
155516383 176649 0 None -154 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4443219 176649 0 None -154 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4598230 176649 0 None -154 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 810 19 7 9 3.5 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
44448606 11886 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 310 6 2 3 2.6 OC(CCCN1CCNCC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1182652 11886 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 310 6 2 3 2.6 OC(CCCN1CCNCC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL258385 11886 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 310 6 2 3 2.6 OC(CCCN1CCNCC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
71718048 86926 0 None 1 2 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 348 4 0 7 1.9 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)c3ccccc3[N+](=O)[O-])C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323443 86926 0 None 1 2 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 348 4 0 7 1.9 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)c3ccccc3[N+](=O)[O-])C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
137635734 156088 0 None -229 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 377 7 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4063176 156088 0 None -229 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 377 7 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
162667844 182509 0 None -3 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 2 0 2 2.8 Cc1ccc2c(c1)CCCN2CC(=O)N1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4787283 182509 0 None -3 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 272 2 0 2 2.8 Cc1ccc2c(c1)CCCN2CC(=O)N1CCCCC1 10.1016/j.bmcl.2020.127632
46227555 14099 1 None -5 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
CHEMBL1198062 14099 1 None -5 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
CHEMBL594376 14099 1 None -5 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@@H]1CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
134149168 148222 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Binding affinity to human M3 receptor expressed in CHO cells measured after 90 mins by radioligand binding assayBinding affinity to human M3 receptor expressed in CHO cells measured after 90 mins by radioligand binding assay
ChEMBL 297 2 0 2 3.6 CN1CC[C@H]2CC(=O)[C@H](Cc3ccccc3)[C@H]3CCC[C@@H]1[C@H]23 10.1016/j.bmcl.2016.10.065
CHEMBL3936289 148222 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Binding affinity to human M3 receptor expressed in CHO cells measured after 90 mins by radioligand binding assayBinding affinity to human M3 receptor expressed in CHO cells measured after 90 mins by radioligand binding assay
ChEMBL 297 2 0 2 3.6 CN1CC[C@H]2CC(=O)[C@H](Cc3ccccc3)[C@H]3CCC[C@@H]1[C@H]23 10.1016/j.bmcl.2016.10.065
4746 204868 31 None -1 4 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL1334033 204868 31 None -1 4 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL75880 204868 31 None -1 4 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
66561967 74675 0 None 1 7 Human 6.2 pKi = 6.2 Binding
Inhibition of M3 muscarinic receptorInhibition of M3 muscarinic receptor
ChEMBL 213 2 0 1 2.0 C1CC2CCC1N2CC12C3C4C5C3C1C5C42 10.1016/j.bmcl.2012.04.077
CHEMBL2030626 74675 0 None 1 7 Human 6.2 pKi = 6.2 Binding
Inhibition of M3 muscarinic receptorInhibition of M3 muscarinic receptor
ChEMBL 213 2 0 1 2.0 C1CC2CCC1N2CC12C3C4C5C3C1C5C42 10.1016/j.bmcl.2012.04.077
611107 203921 1 None -1 3 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 451 7 3 7 0.4 NCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL69287 203921 1 None -1 3 Rat 5.2 pKi = 5.2 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 451 7 3 7 0.4 NCCC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
4189 206899 96 None -12 34 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206899 96 None -12 34 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206899 96 None -12 34 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
53325336 58495 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 353 6 2 4 3.7 NCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683921 58495 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 353 6 2 4 3.7 NCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
11013666 59402 1 None -1 5 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 354 6 0 2 5.2 CN(C)CCC1=C(C(c2ccccc2)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL171102 59402 1 None -1 5 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 354 6 0 2 5.2 CN(C)CCC1=C(C(c2ccccc2)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
156015153 178283 0 None -18 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1105 24 2 10 10.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4641714 178283 0 None -18 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1105 24 2 10 10.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651018 178283 0 None -18 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1105 24 2 10 10.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
44318929 106835 0 None -21 4 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 315 2 0 4 3.1 CN1C2CCCC1C(OC(=O)OCC(Cl)(Cl)Cl)C2 10.1021/jm9904001
CHEMBL314493 106835 0 None -21 4 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 315 2 0 4 3.1 CN1C2CCCC1C(OC(=O)OCC(Cl)(Cl)Cl)C2 10.1021/jm9904001
44299589 196374 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL56275 196374 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@@H]3[C@@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@H]12 10.1016/s0960-894x(02)00315-3
9937474 170446 0 None -3388 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 551 6 1 5 5.3 Nc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4448933 170446 0 None -3388 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 551 6 1 5 5.3 Nc1ccccc1C(=O)N1CCC(N2CCC(Cc3ccc(S(=O)(=O)c4cccc(Cl)c4)cc3)CC2)CC1 10.1016/j.ejmech.2021.113159
11092603 4829 0 None -9 5 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 524 7 0 7 5.8 C=CCOC(=O)c1c(C)n(Cc2ccc(OC)cc2)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL104332 4829 0 None -9 5 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 524 7 0 7 5.8 C=CCOC(=O)c1c(C)n(Cc2ccc(OC)cc2)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
155522355 176385 0 None -5011 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4451030 176385 0 None -5011 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596065 176385 0 None -5011 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 732 19 8 8 2.3 CC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
187 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
137644962 158469 0 None -338 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 363 6 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4091058 158469 0 None -338 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 363 6 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
10418181 9554 1 None -2691 4 Rat 5.2 pKi = 5.2 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 873 26 3 10 8.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL112500 9554 1 None -2691 4 Rat 5.2 pKi = 5.2 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 873 26 3 10 8.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL1201995 9554 1 None -2691 4 Rat 5.2 pKi = 5.2 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 873 26 3 10 8.2 CN(CCCCCCN)CCCCCCCCN(C)CCCCCCN(CC(=O)N1c2ccccc2C(=O)Nc2cccnc21)CC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
176 397 66 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 397 66 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 397 66 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 397 66 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 397 66 None -1 31 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
9815331 203084 1 None -263 8 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
CHEMBL64000 203084 1 None -263 8 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9904001
9815331 203084 1 None -263 8 Rat 6.2 pKi = 6.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 203084 1 None -263 8 Rat 6.2 pKi = 6.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranesInhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
9815331 203084 1 None -263 8 Human 6.2 pKi = 6.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 203084 1 None -263 8 Human 6.2 pKi = 6.2 Binding
Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
187 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
2551 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
162645430 183603 0 None -26 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 860 15 2 7 8.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4744233 183603 0 None -26 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 860 15 2 7 8.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4802409 183603 0 None -26 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 860 15 2 7 8.2 Cc1cc(/C=C/c2cc3c4c(c2)CCCN4CCC3)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
155672 5005 3 None -7 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@@H]1O[C@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL105198 5005 3 None -7 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@@H]1O[C@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL56734 5005 3 None -7 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@@H]1O[C@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
137631026 161126 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 230 1 0 1 3.0 C[N+](C)(C)C1CCc2ccc3ccoc3c2C1 10.1021/acs.jmedchem.7b01113
CHEMBL4093215 161126 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 230 1 0 1 3.0 C[N+](C)(C)C1CCc2ccc3ccoc3c2C1 10.1021/acs.jmedchem.7b01113
CHEMBL4117321 161126 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 230 1 0 1 3.0 C[N+](C)(C)C1CCc2ccc3ccoc3c2C1 10.1021/acs.jmedchem.7b01113
44328347 207528 0 None -3 3 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 317 1 1 2 3.6 OC1(C2=CN3CCC2CC3)c2ccccc2CCc2ccccc21 10.1016/S0960-894X(01)80824-6
CHEMBL94772 207528 0 None -3 3 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity towards muscarinic receptor in parotid gland (M3)In vitro binding affinity towards muscarinic receptor in parotid gland (M3)
ChEMBL 317 1 1 2 3.6 OC1(C2=CN3CCC2CC3)c2ccccc2CCc2ccccc21 10.1016/S0960-894X(01)80824-6
44593621 193273 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524061 193273 0 None -2 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 347 3 0 3 3.7 CN1CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
24894630 188945 0 None -3 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc(C2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL508347 188945 0 None -3 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc(C2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL555475 188945 0 None -3 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc(C2CCC[N+]2(C)C)o1 10.1021/jm800145d
44309231 169474 0 None -7 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 6 2 3 3.7 CCC1(CCN)CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL443267 169474 0 None -7 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 6 2 3 3.7 CCC1(CCN)CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
53322412 58489 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 408 10 1 3 6.7 CCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683916 58489 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 408 10 1 3 6.7 CCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
138710714 177062 0 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 406 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(Br)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4633165 177062 0 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 406 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(Br)cc1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
2705 3813 64 None -1 10 Rat 8.2 pKi = 8.2 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.02.036
360 3813 64 None -1 10 Rat 8.2 pKi = 8.2 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.02.036
443879 3813 64 None -1 10 Rat 8.2 pKi = 8.2 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.02.036
CHEMBL1382 3813 64 None -1 10 Rat 8.2 pKi = 8.2 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.02.036
DB01036 3813 64 None -1 10 Rat 8.2 pKi = 8.2 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1016/j.bmcl.2005.02.036
44627746 14010 0 None -3 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197392 14010 0 None -3 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569760 14010 0 None -3 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
2683 102861 25 None 1 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102861 25 None 1 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102861 25 None 1 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
10484263 58513 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 639 16 6 6 6.5 O=C(Nc1ccccc1-c1ccccc1)NC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683940 58513 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 639 16 6 6 6.5 O=C(Nc1ccccc1-c1ccccc1)NC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
16125619 84694 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 427 5 2 3 4.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(O)c2)CC1 10.1021/jm061159a
CHEMBL222804 84694 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 427 5 2 3 4.3 O=C1NC(c2ccccc2)(c2ccccc2)CN1C1CCN(Cc2cccc(O)c2)CC1 10.1021/jm061159a
16125398 85088 0 None 20 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 442 7 1 2 4.3 C[N+]1(CCOc2ccccc2)CC[C@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL224783 85088 0 None 20 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 442 7 1 2 4.3 C[N+]1(CCOc2ccccc2)CC[C@H](N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
71128 96781 25 None -288 8 Human 8.1 pKi = 8.1 Binding
Antimuscarinic potency and subset specificity was characterised by inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00085a017
CHEMBL26505 96781 25 None -288 8 Human 8.1 pKi = 8.1 Binding
Antimuscarinic potency and subset specificity was characterised by inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by inhibition of the [3H]NMS Binding to Muscarinic acetylcholine receptor M3 subtype
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1021/jm00085a017
59145957 123963 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629358 123963 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution methodDisplacement of [3H]N-methyl scopolamine from human cloned muscarinic M3 receptor by dilution method
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL5289083 194435 0 None -4 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysisDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
ChEMBL 1002 24 3 6 13.3 CN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCCNCCCCCCN3CCC(COC(=O)Nc4ccc(F)cc4-c4ccc(F)c(Cl)c4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.2c01376
3652 4066 79 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 4066 79 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 4066 79 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 4066 79 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 4066 79 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
44627740 198735 0 None -6 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL583051 198735 0 None -6 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 339 4 1 3 4.9 CN1CCCC1c1ccc(C(O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
134272503 176387 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 9 1 4 4.7 COc1ccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)cc1 10.1016/j.bmc.2019.06.016
CHEMBL4545504 176387 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 9 1 4 4.7 COc1ccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)cc1 10.1016/j.bmc.2019.06.016
CHEMBL4596068 176387 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 486 9 1 4 4.7 COc1ccc(CCC[N+]23CCC(CC2)C(OC(=O)C(O)(c2ccccc2)c2ccccc2)C3)cc1 10.1016/j.bmc.2019.06.016
10646906 119207 0 None -2 3 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 443 6 3 4 3.7 Nc1ccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)cc1 10.1021/jm0003135
CHEMBL343449 119207 0 None -2 3 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 443 6 3 4 3.7 Nc1ccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)cc1 10.1021/jm0003135
44406321 72749 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 415 3 1 3 4.3 CO[C@]1(C#CC(O)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL199981 72749 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 415 3 1 3 4.3 CO[C@]1(C#CC(O)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44406395 140255 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 375 3 1 3 3.7 CO[C@]1(C#CC(O)(c2cccc(C)c2)c2cccc(C)c2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL380583 140255 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 375 3 1 3 3.7 CO[C@]1(C#CC(O)(c2cccc(C)c2)c2cccc(C)c2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
44406689 141260 0 None 5 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 349 3 1 5 1.8 COC1(C#CC(O)(c2ccccc2)c2cccnn2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
CHEMBL383248 141260 0 None 5 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 349 3 1 5 1.8 COC1(C#CC(O)(c2ccccc2)c2cccnn2)CN2CCC1CC2 10.1016/j.bmcl.2005.09.079
16125621 84334 0 None 22 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 426 5 2 3 4.2 Nc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
CHEMBL221829 84334 0 None 22 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 426 5 2 3 4.2 Nc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
44409751 74414 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2CCC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL202729 74414 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 4.0 Cc1c(NC2CCC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
44409945 140139 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 3.9 Cc1c(N[C@H]2C[C@@H]2C)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL380314 140139 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 300 4 1 4 3.9 Cc1c(N[C@H]2C[C@@H]2C)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL5069430 214194 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CN(C(=O)O[C@H]3CN4CCC3CC4)c3cccnc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5074216 214292 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@@H]3CCN(C)C3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
90200594 190657 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 477 8 2 7 3.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)O)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5181855 190657 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 477 8 2 7 3.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)O)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
134346261 191565 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 492 8 2 6 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2csc(C(=O)O)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5195224 191565 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 492 8 2 6 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2csc(C(=O)O)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
86720815 192035 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 486 8 2 5 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5202567 192035 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 486 8 2 5 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)O)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
86720819 192054 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 486 8 2 5 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cccc(C(=O)O)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5202787 192054 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysisDisplacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
ChEMBL 486 8 2 5 4.9 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cccc(C(=O)O)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
118737359 119040 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426707 119040 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
9913892 205814 0 None 100 2 Human 8.1 pKi = 8.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 499 6 0 5 5.7 O=C(c1ccc([N+](=O)[O-])s1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL83459 205814 0 None 100 2 Human 8.1 pKi = 8.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 499 6 0 5 5.7 O=C(c1ccc([N+](=O)[O-])s1)N(c1ccc(Br)cc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
155518181 170237 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 404 4 0 3 5.2 O=C(OCc1ccc(Cl)c(Cl)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4446039 170237 0 None -1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 404 4 0 3 5.2 O=C(OCc1ccc(Cl)c(Cl)c1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
10203251 5192 0 None -35 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 434 5 0 6 4.8 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(OC)cc2CCN1C3 10.1021/jm011116o
CHEMBL106224 5192 0 None -35 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 434 5 0 6 4.8 CCCc1c(C(=O)OCC)c2c3c(ccc2n1C)OC1c2ccc(OC)cc2CCN1C3 10.1021/jm011116o
9931930 108573 0 None -35 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 5 1 5 4.8 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL320465 108573 0 None -35 5 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 420 5 1 5 4.8 CCCc1[nH]c2ccc3c(c2c1C(=O)OCC)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
10770914 25029 0 None -239 5 Rat 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 691 25 3 7 6.4 CN(CCCCCCCCN(C)C(=O)CCCCCNCCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
CHEMBL134692 25029 0 None -239 5 Rat 7.2 pKi = 7.2 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 691 25 3 7 6.4 CN(CCCCCCCCN(C)C(=O)CCCCCNCCCCC(=O)N1c2ccccc2C(=O)Nc2cccnc21)C(=O)CCCCCN 10.1021/jm981038d
9894173 15118 4 None -776 5 Human 6.2 pKi = 6.2 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 565 6 1 5 5.6 Cc1cccc(C(=O)N2CCC(N3CCC(Cc4ccc(S(=O)(=O)c5cccc(Cl)c5)cc4)CC3)CC2)c1N 10.1021/jm301774u
CHEMBL12098 15118 4 None -776 5 Human 6.2 pKi = 6.2 Binding
Binding affinity to human M3 muscarinic receptorBinding affinity to human M3 muscarinic receptor
ChEMBL 565 6 1 5 5.6 Cc1cccc(C(=O)N2CCC(N3CCC(Cc4ccc(S(=O)(=O)c5cccc(Cl)c5)cc4)CC3)CC2)c1N 10.1021/jm301774u
2551 791 23 None -54 11 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
44377401 56512 1 None - 1 Rat 6.2 pKi = 6.2 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 293 9 1 3 1.8 CN(CC#CCN1CCCC1)C(=O)CCCCCCCN 10.1021/jm00164a044
CHEMBL1202134 56512 1 None - 1 Rat 6.2 pKi = 6.2 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 293 9 1 3 1.8 CN(CC#CCN1CCCC1)C(=O)CCCCCCCN 10.1021/jm00164a044
CHEMBL163875 56512 1 None - 1 Rat 6.2 pKi = 6.2 Binding
Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cellsMuscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
ChEMBL 293 9 1 3 1.8 CN(CC#CCN1CCCC1)C(=O)CCCCCCCN 10.1021/jm00164a044
44207909 16667 3 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
CHEMBL1242923 16667 3 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
10969390 59647 0 None -97 6 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 324 7 0 2 4.5 CC(C1=C(CCN(C)CCF)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL172233 59647 0 None -97 6 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 324 7 0 2 4.5 CC(C1=C(CCN(C)CCF)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
187 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
294 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
65 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
8593 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
CHEMBL667 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
DB03128 255 39 None -26 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2007.11.073
137636308 156178 0 None -22 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 329 7 0 3 2.8 CCCCN1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4064222 156178 0 None -22 8 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 329 7 0 3 2.8 CCCCN1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
44448530 12303 0 None 1 2 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 386 7 1 3 4.5 OC(CCCN1CCN(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185259 12303 0 None 1 2 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 386 7 1 3 4.5 OC(CCCN1CCN(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL403029 12303 0 None 1 2 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 386 7 1 3 4.5 OC(CCCN1CCN(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
44443734 94210 0 None 16 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 382 7 2 3 3.5 CC(C)=CCCN1C[C@H]2[C@H](NC(=O)[C@@](O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
CHEMBL250031 94210 0 None 16 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 382 7 2 3 3.5 CC(C)=CCCN1C[C@H]2[C@H](NC(=O)[C@@](O)(c3ccccc3)C3CCCC3)[C@H]2C1 10.1016/j.bmcl.2007.06.081
71720489 86930 0 None 1 2 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 303 3 0 5 2.0 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)c3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323447 86930 0 None 1 2 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 303 3 0 5 2.0 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)c3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
57326325 77155 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042554 77155 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078987 77155 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1021/jm2013216
57326325 77155 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL2042554 77155 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
CHEMBL2078987 77155 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
ChEMBL 297 4 0 3 2.9 CN(C)C[C@@H]1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2017.06.004
5318 15544 49 None -1 13 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1200348 15544 49 None -1 13 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1221 15544 49 None -1 13 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
11498 2997 41 None -38 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/j.bmcl.2008.03.061
4995951 2997 41 None -38 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/j.bmcl.2008.03.061
CHEMBL59898 2997 41 None -38 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC 10.1016/j.bmcl.2008.03.061
44448421 12305 0 None -9 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 616 13 2 4 7.8 OC(CCCN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185269 12305 0 None -9 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 616 13 2 4 7.8 OC(CCCN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL403773 12305 0 None -9 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 616 13 2 4 7.8 OC(CCCN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
162675053 183234 0 None -11 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 5 1 3 3.2 O=C(CCN1CCCc2ccccc21)NCc1cccs1 10.1016/j.bmcl.2020.127632
CHEMBL4796491 183234 0 None -11 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 300 5 1 3 3.2 O=C(CCN1CCCc2ccccc21)NCc1cccs1 10.1016/j.bmcl.2020.127632
156012563 178224 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4637485 178224 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650635 178224 0 None -3 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccccc2)CO1 10.1021/acs.jmedchem.9b02100
156015045 178241 0 None -17 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4648218 178241 0 None -17 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650765 178241 0 None -17 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 376 5 0 4 2.7 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(S(=O)(=O)c3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
44274432 80098 0 None -5 5 Human 4.1 pKi = 4.1 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 333 5 0 3 3.0 CN(C)CCN(C)C(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
CHEMBL21328 80098 0 None -5 5 Human 4.1 pKi = 4.1 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 333 5 0 3 3.0 CN(C)CCN(C)C(=O)C1=C/C(=C\c2cccnc2)c2ccccc21 10.1016/s0960-894x(01)00186-x
16125529 137181 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 412 5 1 1 4.4 C[N+]1(Cc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL374987 137181 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 412 5 1 1 4.4 C[N+]1(Cc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
44437249 11840 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 235 3 0 3 1.6 Cc1cc(OCC#CC[N+]2(C)CCCC2)no1 10.1016/j.bmc.2007.09.003
CHEMBL1182436 11840 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 235 3 0 3 1.6 Cc1cc(OCC#CC[N+]2(C)CCCC2)no1 10.1016/j.bmc.2007.09.003
CHEMBL238825 11840 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 235 3 0 3 1.6 Cc1cc(OCC#CC[N+]2(C)CCCC2)no1 10.1016/j.bmc.2007.09.003
24882532 95088 0 None -5 5 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cells
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL255523 95088 0 None -5 5 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M3 receptor expressed in CHO cells
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
44318817 169090 0 None -32 4 Human 5.1 pKi = 5.1 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 197 2 0 3 1.6 CCC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
CHEMBL440138 169090 0 None -32 4 Human 5.1 pKi = 5.1 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 197 2 0 3 1.6 CCC(=O)OC1CC2CCCC1N2C 10.1021/jm9904001
11808947 59423 0 None -14 5 Human 6.1 pKi = 6.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 CC(C1=C(CN(C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
CHEMBL171216 59423 0 None -14 5 Human 6.1 pKi = 6.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 306 5 0 2 4.5 CC(C1=C(CN(C)C(C)C)Cc2ccccc21)c1ccccn1 10.1021/jm020895l
108993425 181734 1 None -19 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 2 0 2 2.1 O=C(CN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4777543 181734 1 None -19 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 2 0 2 2.1 O=C(CN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
44448575 11885 0 None 1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 3 3.0 CN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182650 11885 0 None 1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 3 3.0 CN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL258161 11885 0 None 1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 324 6 1 3 3.0 CN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
156015978 178299 0 None -35 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4636899 178299 0 None -35 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651111 178299 0 None -35 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL69452 203951 0 None -4 5 Human 5.1 pKi = 5.1 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 331 6 1 5 2.7 CCO/C(O)=C1\CN2CC(CCC2COCc2ccccc2)C1=O 10.1021/jm020572p
44318766 205728 0 None -5 4 Human 5.1 pKi = 5.1 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 237 2 1 3 2.4 O=C(OC1CC2CCCC1N2)C1CCCCC1 10.1021/jm9904001
CHEMBL82754 205728 0 None -5 4 Human 5.1 pKi = 5.1 Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranesInhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
ChEMBL 237 2 1 3 2.4 O=C(OC1CC2CCCC1N2)C1CCCCC1 10.1021/jm9904001
137644950 158468 0 None -1 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 4 0 3 1.6 CN1CCC(COCc2cccnc2)C1 10.1021/acs.jmedchem.7b01113
CHEMBL4091032 158468 0 None -1 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 206 4 0 3 1.6 CN1CCC(COCc2cccnc2)C1 10.1021/acs.jmedchem.7b01113
164623076 188543 0 None -1995 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4872608 188543 0 None -1995 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028732 188543 0 None -1995 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 888 22 9 12 0.6 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NCCN1CCN(CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
24865895 95976 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL259662 95976 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL390842 95976 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
44448496 11880 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 401 7 1 2 4.7 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL1182637 11880 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 401 7 1 2 4.7 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
CHEMBL257547 11880 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 401 7 1 2 4.7 C[N+]1(CCCC(O)(c2ccccc2)c2ccccc2)CCN(c2ccccc2)CC1 10.1016/j.bmcl.2008.03.061
44422692 11821 0 None -5 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL1182296 11821 0 None -5 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
CHEMBL228144 11821 0 None -5 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmcl.2007.11.073
24865895 95976 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL259662 95976 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
CHEMBL390842 95976 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2009.10.027
24865895 95976 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
CHEMBL259662 95976 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
CHEMBL390842 95976 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysisDisplacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmcl.2014.06.020
44309135 96539 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 7 2 3 3.7 NCCCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL263040 96539 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 7 2 3 3.7 NCCCCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
90666109 109312 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(O)cc(F)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219039 109312 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(O)cc(F)c3)CC2)ccc1O 10.1039/C1MD00140J
44247935 196554 0 None -234 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 294 5 0 3 4.1 C[C@@H](c1ccccn1)c1c(CCN(C)C)oc2ccccc12 10.1021/jm900933k
CHEMBL563920 196554 0 None -234 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO Flp-In cells by liquid scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO Flp-In cells by liquid scintillation counting
ChEMBL 294 5 0 3 4.1 C[C@@H](c1ccccn1)c1c(CCN(C)C)oc2ccccc12 10.1021/jm900933k
1209 1645 75 None -30 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
203 1645 75 None -30 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
3386 1645 75 None -30 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
CHEMBL41 1645 75 None -30 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
DB00472 1645 75 None -30 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
2551 791 23 None -54 11 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
53317169 58484 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 338 5 1 3 4.8 CCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683911 58484 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 338 5 1 3 4.8 CCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
44593627 193275 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL524071 193275 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
CHEMBL541671 193275 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 362 3 0 2 3.8 C[N+]1(C)CCC[C@H]1[C@H]1C[S+]([O-])[C@](c2ccccc2)(C2CCCCC2)O1 10.1016/j.bmc.2008.04.013
46905988 91930079 10384 0 None 3 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 8 2 3 3.7 O=C(N[C@H]1[C@@H]2CN(CCCc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL1162964 10384 0 None 3 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 418 8 2 3 3.7 O=C(N[C@H]1[C@@H]2CN(CCCc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
132712 171774 19 None -25 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL 567 10 1 5 6.1 CCCC(C)(C)C(=O)N(CC)CCCC1CCN(CC(=O)N2c3ccc(Cl)cc3C(=O)Nc3cccnc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4468100 171774 19 None -25 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL 567 10 1 5 6.1 CCCC(C)(C)C(=O)N(CC)CCCC1CCN(CC(=O)N2c3ccc(Cl)cc3C(=O)Nc3cccnc32)CC1 10.1021/acs.jmedchem.8b01967
155560140 176323 0 None -524 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4565234 176323 0 None -524 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4595575 176323 0 None -524 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 789 21 9 9 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
36014865 182646 2 None -6 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 280 4 1 2 3.5 O=C(CCN1CCCc2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2020.127632
CHEMBL4789054 182646 2 None -6 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 280 4 1 2 3.5 O=C(CCN1CCCc2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2020.127632
71128 96781 25 None -288 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
CHEMBL26505 96781 25 None -288 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.01.072
137629935 160996 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4060823 160996 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116342 160996 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
24894637 188695 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL504733 188695 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
CHEMBL553434 188695 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 180 1 0 1 2.5 Cc1ccc([C@H]2CCC[N+]2(C)C)o1 10.1021/jm800145d
46227459 14103 0 None 1 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
CHEMBL1198076 14103 0 None 1 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
CHEMBL594802 14103 0 None 1 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 188 2 0 2 0.9 CC1(C)CO[C@H](C[N+](C)(C)C)CO1 10.1016/j.bmc.2009.10.027
611037 203671 1 None -1 4 Rat 7.1 pKi = 7.1 Binding
The compound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M3 of transfected A9L cells.The compound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M3 of transfected A9L cells.
ChEMBL 399 4 1 5 2.2 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCl)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL67532 203671 1 None -1 4 Rat 7.1 pKi = 7.1 Binding
The compound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M3 of transfected A9L cells.The compound was tested for the inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M3 of transfected A9L cells.
ChEMBL 399 4 1 5 2.2 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCCl)CC2)c2ccccc21 10.1021/jm00111a032
118500 156975 63 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 165 4 1 2 1.5 CNCCc1cccc(OC)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4073256 156975 63 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 165 4 1 2 1.5 CNCCc1cccc(OC)c1 10.1021/acs.jmedchem.7b01113
137629935 160996 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4060823 160996 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116342 160996 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
10381417 68639 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 321 5 1 2 4.6 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@H]3C2C)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
CHEMBL192061 68639 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 321 5 1 2 4.6 Cc1ccc(O)c(C(CCN2C[C@H]3C[C@H]3C2C)c2ccccc2)c1 10.1016/j.bmcl.2005.02.036
44430472 86974 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 272 3 0 4 2.9 c1c(N2CCCCCC2)nc(C2CC2)nc1N1CCC1 10.1016/j.bmcl.2007.03.047
CHEMBL232416 86974 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 272 3 0 4 2.9 c1c(N2CCCCCC2)nc(C2CC2)nc1N1CCC1 10.1016/j.bmcl.2007.03.047
44430456 168380 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 314 3 0 4 4.0 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCCCC1 10.1016/j.bmcl.2007.03.047
CHEMBL434765 168380 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 314 3 0 4 4.0 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CCCCC1 10.1016/j.bmcl.2007.03.047
44409937 75966 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 287 4 2 5 2.9 Nc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205482 75966 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 287 4 2 5 2.9 Nc1c(NC2CC2)nc(C2CC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
44409982 76218 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 314 4 1 4 4.4 Cc1c(NC2CC2)nc(C2CCCC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205841 76218 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 314 4 1 4 4.4 Cc1c(NC2CC2)nc(C2CCCC2)nc1N1CCCCCC1 10.1016/j.bmcl.2006.01.006
10236419 76245 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 290 4 1 5 2.8 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCSCC1 10.1016/j.bmcl.2006.01.006
CHEMBL205853 76245 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 290 4 1 5 2.8 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCSCC1 10.1016/j.bmcl.2006.01.006
44409754 76675 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 284 4 1 4 3.4 C=C1CCN(c2nc(C3CC3)nc(NC3CC3)c2C)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL206480 76675 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 284 4 1 4 3.4 C=C1CCN(c2nc(C3CC3)nc(NC3CC3)c2C)CC1 10.1016/j.bmcl.2006.01.006
44409978 140166 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 314 7 2 5 4.0 Cc1c(NCCc2cccs2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
CHEMBL380477 140166 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 314 7 2 5 4.0 Cc1c(NCCc2cccs2)nc(C2CC2)nc1NC1CC1 10.1016/j.bmcl.2006.01.006
44379080 58135 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 678 10 0 5 7.5 CCN(CCCCC1CCN(CC(=O)N2c3ccccc3C(=O)N(C(=O)c3ccc(F)cc3)c3ccccc32)CC1)C(=O)c1ccc(F)cc1 10.1016/S0960-894X(97)00109-1
CHEMBL168149 58135 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)Tested in vitro for the binding affinity against muscarinic receptor subtype 3 (M3)
ChEMBL 678 10 0 5 7.5 CCN(CCCCC1CCN(CC(=O)N2c3ccccc3C(=O)N(C(=O)c3ccc(F)cc3)c3ccccc32)CC1)C(=O)c1ccc(F)cc1 10.1016/S0960-894X(97)00109-1
3652 4066 79 None -3 18 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
57 4066 79 None -3 18 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
60809 4066 79 None -3 18 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
CHEMBL21536 4066 79 None -3 18 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
DB15357 4066 79 None -3 18 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
9909908 13487 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 381 14 1 6 4.5 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCO)C1 10.1021/jm0301235
CHEMBL1193635 13487 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 381 14 1 6 4.5 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCO)C1 10.1021/jm0301235
CHEMBL545077 13487 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 381 14 1 6 4.5 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCO)C1 10.1021/jm0301235
11071537 26465 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 495 17 0 10 5.5 COc1nsnc1OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL136027 26465 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Compound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cellsCompound was tested for binding inhibition of [3H](R)-QNB to Muscarinic acetylcholine receptor M3 expressed in A9 L cells
ChEMBL 495 17 0 10 5.5 COc1nsnc1OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
2396803 206103 3 None 10 2 Human 7.1 pKi = 7.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 398 7 0 2 5.3 O=C(CCc1ccccc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL85950 206103 3 None 10 2 Human 7.1 pKi = 7.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 398 7 0 2 5.3 O=C(CCc1ccccc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
3652 4066 79 None -3 18 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4066 79 None -3 18 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4066 79 None -3 18 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4066 79 None -3 18 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4066 79 None -3 18 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M3 receptor expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
44409660 75907 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 362 6 1 4 4.7 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(Cc2ccccc2)CC1 10.1016/j.bmcl.2006.01.006
CHEMBL205140 75907 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cellsDisplacement of [3H]methylscopolamine from recombinant human muscarinic M3 receptors expressed in CHO cells
ChEMBL 362 6 1 4 4.7 Cc1c(NC2CC2)nc(C2CC2)nc1N1CCC(Cc2ccccc2)CC1 10.1016/j.bmcl.2006.01.006
44430466 93272 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 311 3 0 5 3.0 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(C#N)C1 10.1016/j.bmcl.2007.03.047
CHEMBL245137 93272 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membraneDisplacement of [3H]N-methylscopolamine from human recombinant M3 muscarinic receptor expressed in CHO cell membrane
ChEMBL 311 3 0 5 3.0 Cc1c(N2CCCCCC2)nc(C2CC2)nc1N1CC(C#N)C1 10.1016/j.bmcl.2007.03.047
44299564 199064 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
CHEMBL58824 199064 0 None 1 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@H]2C[C@H]3CCCC[C@H]3[C@H](/C=C\[C@H]3CCC[C@H](C)N3C)[C@@H]12 10.1016/s0960-894x(02)00315-3
44318781 106951 0 None 5 2 Human 6.1 pKi = 6.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 415 6 0 4 4.9 O=C(c1ccc([N+](=O)[O-])cc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
CHEMBL315127 106951 0 None 5 2 Human 6.1 pKi = 6.1 Binding
In vitro affinity for muscarinic M3 receptor.In vitro affinity for muscarinic M3 receptor.
ChEMBL 415 6 0 4 4.9 O=C(c1ccc([N+](=O)[O-])cc1)N(c1ccccc1)C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(02)00487-0
14939894 10264 0 None -467 4 Rat 6.1 pKi = 6.1 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 742 28 3 8 8.0 COc1ccccc1CNCCCCCCN(C)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
CHEMBL116172 10264 0 None -467 4 Rat 6.1 pKi = 6.1 Binding
Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMSTested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS
ChEMBL 742 28 3 8 8.0 COc1ccccc1CNCCCCCCN(C)CCCCCCCCN(C)CCCCCCNCC(=O)N1c2ccccc2C(=O)Nc2cccnc21 10.1021/jm00046a021
2736067 87501 73 None -93 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from recombinant muscarinic M3 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-NMS from recombinant muscarinic M3 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysis
ChEMBL 230 1 1 2 2.4 Clc1cc(Cl)cc(N2CCNCC2)c1 10.1021/jm400140q
CHEMBL2335158 87501 73 None -93 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from recombinant muscarinic M3 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-NMS from recombinant muscarinic M3 receptor (unknown origin) expressed in CHOK1 cells after 60 mins by liquid scintillation counting analysis
ChEMBL 230 1 1 2 2.4 Clc1cc(Cl)cc(N2CCNCC2)c1 10.1021/jm400140q
108993439 179836 1 None -3 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 2 0 2 2.1 CC1Cc2ccccc2N1CC(=O)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4745429 179836 1 None -3 4 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 244 2 0 2 2.1 CC1Cc2ccccc2N1CC(=O)N1CCCC1 10.1016/j.bmcl.2020.127632
44339221 8693 0 None - 1 Rat 4.1 pKi = 4.1 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary glandThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary gland
ChEMBL 220 2 0 3 2.0 CCC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
CHEMBL109593 8693 0 None - 1 Rat 4.1 pKi = 4.1 Binding
The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary glandThe compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in submandibular salivary gland
ChEMBL 220 2 0 3 2.0 CCC#CCON=C1CC2CCC(C1)N2C 10.1021/jm9708588
155562285 175818 0 None 1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CN3CCC2CC3)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
CHEMBL4585326 175818 0 None 1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 380 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CN3CCC2CC3)c2ccccc2)cc1 10.1016/j.bmcl.2018.12.022
26987 946 33 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 946 33 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 946 33 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 946 33 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 946 33 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
44308746 203828 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 352 3 2 3 2.6 CC1(N)CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL68609 203828 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 352 3 2 3 2.6 CC1(N)CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
90666110 109314 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)c(O)cc3F)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219041 109314 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)c(O)cc3F)CC2)ccc1O 10.1039/C1MD00140J
71452792 79624 0 None -1 2 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1[C@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00090a006
CHEMBL2115125 79624 0 None -1 2 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cellInhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
ChEMBL 335 4 0 3 3.6 CN1CC2CC1[C@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00090a006
410345 89774 4 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 333 8 1 4 3.4 CCN(CC)CCOC(=O)C(c1ccccc1)C1(O)CCCCC1 10.1016/j.bmc.2013.01.072
CHEMBL2377269 89774 4 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
ChEMBL 333 8 1 4 3.4 CCN(CC)CCOC(=O)C(c1ccccc1)C1(O)CCCCC1 10.1016/j.bmc.2013.01.072
16125571 85121 0 None 79 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 6 1 3 4.6 COc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
CHEMBL225074 85121 0 None 79 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 6 1 3 4.6 COc1cccc(CN2CCC(N3CC(c4ccccc4)(c4ccccc4)NC3=O)CC2)c1 10.1021/jm061159a
90666121 109328 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 742 18 6 9 7.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C3CCC2CC(OC(=O)Nc2ccccc2-c2ccc(O)c(Cl)c2)C3)ccc1O 10.1039/C1MD00140J
CHEMBL3219054 109328 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 742 18 6 9 7.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C3CCC2CC(OC(=O)Nc2ccccc2-c2ccc(O)c(Cl)c2)C3)ccc1O 10.1039/C1MD00140J
10718110 39885 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 443 6 2 4 3.8 Cc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)n1 10.1021/jm0003135
CHEMBL147778 39885 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 443 6 2 4 3.8 Cc1cccc(CN2CCC(NC(=O)[C@](O)(c3ccccc3)[C@@H]3CCC(F)(F)C3)CC2)n1 10.1021/jm0003135
44627852 14007 0 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 338 4 0 1 5.9 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197387 14007 0 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 338 4 0 1 5.9 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL569712 14007 0 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 338 4 0 1 5.9 C[N+]1(C)CCCC1c1ccc(C(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
2335 11816 22 None -1 12 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
8478 11816 22 None -1 12 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL1182210 11816 22 None -1 12 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
CHEMBL221753 11816 22 None -1 12 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 nan
134271233 176515 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 428 6 1 3 4.3 O=C(OC1C[N+]2(Cc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4591883 176515 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 428 6 1 3 4.3 O=C(OC1C[N+]2(Cc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
CHEMBL4597134 176515 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting methodDisplacement of [3H]NMS from human M3R expressed in CHOK1 cell membranes incubated for 2 hrs by microbeta scintillation counting method
ChEMBL 428 6 1 3 4.3 O=C(OC1C[N+]2(Cc3ccccc3)CCC1CC2)C(O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2019.06.016
156015807 178275 0 None -63 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4641726 178275 0 None -63 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650973 178275 0 None -63 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
162677523 183650 0 None -104 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 930 14 2 10 5.8 CN(C)c1ccc2c(-c3ccc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
CHEMBL4756833 183650 0 None -104 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 930 14 2 10 5.8 CN(C)c1ccc2c(-c3ccc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
CHEMBL4802932 183650 0 None -104 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 930 14 2 10 5.8 CN(C)c1ccc2c(-c3ccc(C(=O)NCCN4CCN(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)CC4)cc3C(=O)[O-])c3ccc(=[N+](C)C)cc-3oc2c1 10.1039/d0md00137f
170332 160952 1 None -7 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4091934 160952 1 None -7 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115997 160952 1 None -7 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
11001809 59051 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 4 2.7 CN(C)CCOC(=O)C1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL169594 59051 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 4 2.7 CN(C)CCOC(=O)C1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
11011332 120776 1 None -2 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
CHEMBL355560 120776 1 None -2 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 278 5 0 2 3.6 CN(C)CCC1=C(Cc2cccnc2)c2ccccc2C1 10.1021/jm020895l
170332 160952 1 None -7 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4091934 160952 1 None -7 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115997 160952 1 None -7 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M3 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
57326142 77151 0 None -4 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL2042401 77151 0 None -4 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
CHEMBL2078965 77151 0 None -4 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 188 3 0 2 0.9 CC[C@@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1021/jm2013216
24894515 176846 4 None -1 5 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@@H]1c1ccco1 10.1021/jm800145d
CHEMBL461502 176846 4 None -1 5 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counterDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by liquid scintillation counter
ChEMBL 151 1 0 2 2.0 CN1CCC[C@@H]1c1ccco1 10.1021/jm800145d
16125371 84730 0 None 28 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 397 5 1 2 4.2 O=C1NC(c2ccccc2)(c2ccccc2)CN1[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm061159a
CHEMBL223017 84730 0 None 28 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 397 5 1 2 4.2 O=C1NC(c2ccccc2)(c2ccccc2)CN1[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm061159a
44622849 196768 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of muscarinic receptor 3Inhibition of muscarinic receptor 3
ChEMBL 293 2 1 5 1.7 Cc1nc2c3c(nc(Cc4ccccc4)n2n1)CCNCC3 10.1016/j.bmcl.2009.07.063
CHEMBL565547 196768 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of muscarinic receptor 3Inhibition of muscarinic receptor 3
ChEMBL 293 2 1 5 1.7 Cc1nc2c3c(nc(Cc4ccccc4)n2n1)CCNCC3 10.1016/j.bmcl.2009.07.063
49783209 17577 0 None -1445 27 Human 6.1 pKi = 6.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17577 0 None -1445 27 Human 6.1 pKi = 6.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
135398745 2893 112 None -27 66 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2893 112 None -27 66 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2893 112 None -27 66 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2893 112 None -27 66 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
16125570 142291 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 6 1 3 4.6 COc1ccccc1CN1CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061159a
CHEMBL388541 142291 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 441 6 1 3 4.6 COc1ccccc1CN1CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061159a
9794266 157127 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 205 2 0 2 2.1 COc1cccc2c1CC(N(C)C)CC2 10.1021/acs.jmedchem.7b01113
CHEMBL4075227 157127 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 205 2 0 2 2.1 COc1cccc2c1CC(N(C)C)CC2 10.1021/acs.jmedchem.7b01113
11184481 201405 15 None -2 4 Human 5.1 pKi = 5.1 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 258 1 0 5 1.8 Cc1ccc2oc(N3CCN4CCC3CC4)nc2n1 10.1021/jm9015075
CHEMBL604798 201405 15 None -2 4 Human 5.1 pKi = 5.1 Binding
Inhibition of muscarinic M3 receptorInhibition of muscarinic M3 receptor
ChEMBL 258 1 0 5 1.8 Cc1ccc2oc(N3CCN4CCC3CC4)nc2n1 10.1021/jm9015075
71718668 86770 0 None 1 2 Rat 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 337 3 0 5 2.7 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)c3ccccc3Cl)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2321893 86770 0 None 1 2 Rat 4.1 pKi = 4.1 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 337 3 0 5 2.7 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)c3ccccc3Cl)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
53325044 58496 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 367 7 2 4 4.1 NCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683922 58496 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 367 7 2 4 4.1 NCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
149706871 177613 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 358 5 2 4 4.0 COc1ccc(-c2cc(F)ccc2NC(=O)OCC2CCNCC2)cc1 10.1021/acs.jmedchem.0c00297
CHEMBL4641288 177613 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting methodDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
ChEMBL 358 5 2 4 4.0 COc1ccc(-c2cc(F)ccc2NC(=O)OCC2CCNCC2)cc1 10.1021/acs.jmedchem.0c00297
CHEMBL69452 203951 0 None -4 5 Human 6.1 pKi = 6.1 Binding
Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligandBinding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand
ChEMBL 331 6 1 5 2.7 CCO/C(O)=C1\CN2CC(CCC2COCc2ccccc2)C1=O 10.1021/jm020572p
156015141 178243 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 668 11 1 4 8.2 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4642045 178243 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 668 11 1 4 8.2 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.9b02172
CHEMBL4650774 178243 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 668 11 1 4 8.2 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.9b02172
156015254 178263 0 None -19 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 984 19 2 7 10.6 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4649420 178263 0 None -19 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 984 19 2 7 10.6 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650938 178263 0 None -19 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 984 19 2 7 10.6 C[N+]1=C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccccc3C2(C)C)C(C)(C)c2ccccc21 10.1021/acs.jmedchem.9b02172
44627741 197659 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 317 4 0 2 5.2 CN1CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL571123 197659 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 317 4 0 2 5.2 CN1CCCC1c1ccc(C(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
162654942 183647 0 None -44 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 833 17 2 7 8.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4754371 183647 0 None -44 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 833 17 2 7 8.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
CHEMBL4802913 183647 0 None -44 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
ChEMBL 833 17 2 7 8.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1 10.1039/d0md00137f
2229 463 22 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 10.1021/jm0510878
295 463 22 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 10.1021/jm0510878
CHEMBL128365 463 22 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cellsBinding affinity to cloned human muscarinic M3 receptor expressed in CHO cells
ChEMBL 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 10.1021/jm0510878
164620907 188524 0 None -10232 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 917 22 10 13 -0.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4865939 188524 0 None -10232 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 917 22 10 13 -0.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028619 188524 0 None -10232 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 917 22 10 13 -0.9 CC(=O)N[C@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
162353374 180019 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.2 CC1CCCCN1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
CHEMBL4747590 180019 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.2 CC1CCCCN1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
162353394 180746 0 None -1 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 245 2 0 3 1.5 O=C(CN1CCCc2cnccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4756237 180746 0 None -1 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 245 2 0 3 1.5 O=C(CN1CCCc2cnccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
156015895 178257 0 None -6 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 993 21 2 8 10.7 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4643290 178257 0 None -6 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 993 21 2 8 10.7 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650874 178257 0 None -6 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assayDisplacement of [3H]-NMS from human muscarinic M3 receptor stably expressed in CHO-K9 cells by radioligand competitive binding assay
ChEMBL 993 21 2 8 10.7 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCCCC3CCN(CC(=O)N4c5ccccc5NC(=O)c5ccccc54)CC3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
137636830 161200 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 4 0 1 2.5 COc1cccc(C2CC2C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4061384 161200 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 4 0 1 2.5 COc1cccc(C2CC2C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4117956 161200 0 None -1 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methyl-scopolamine bromide from human recombinant muscarinic M3 receptor expressed in HEK293T cell membranes after 1 hr by liquid scintillation counting method
ChEMBL 220 4 0 1 2.5 COc1cccc(C2CC2C[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
44448498 12307 0 None -3 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 534 12 2 4 6.0 OC(CCCN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185287 12307 0 None -3 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 534 12 2 4 6.0 OC(CCCN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL404866 12307 0 None -3 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cellsDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells
ChEMBL 534 12 2 4 6.0 OC(CCCN1CCN(CCCC(O)(c2ccccc2)c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
2284 3160 33 None -10 29 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3160 33 None -10 29 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3160 33 None -10 29 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3160 33 None -10 29 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3160 33 None -10 29 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
44437308 12295 0 None -1 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 285 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc2C1 10.1016/j.bmc.2007.09.003
CHEMBL1185188 12295 0 None -1 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 285 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc2C1 10.1016/j.bmc.2007.09.003
CHEMBL396845 12295 0 None -1 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cellsDisplacement of [3H]QNB from human muscarinic M3 receptor expressed in CHO cells
ChEMBL 285 2 0 3 1.9 C[N+]1(CC#CCOC2=NOCC2)CCc2ccccc2C1 10.1016/j.bmc.2007.09.003
44309090 203726 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 366 6 3 3 2.8 O=C(NCCC1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
CHEMBL67873 203726 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 366 6 3 3 2.8 O=C(NCCC1CCNCC1)[C@](O)(c1ccccc1)[C@@H]1CCC(F)(F)C1 10.1016/s0960-894x(03)00350-0
57339144 92209 78 None -12 6 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM3Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM3
ChEMBL 529 6 1 5 4.8 O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1 10.6019/CHEMBL5212743
CHEMBL2426364 92209 78 None -12 6 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM3Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM3
ChEMBL 529 6 1 5 4.8 O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1 10.6019/CHEMBL5212743
11809446 59649 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 4 2.7 CN(C)CCOC(=O)C1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL172234 59649 0 None -1 5 Human 5.1 pKi = 5.1 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 322 6 0 4 2.7 CN(C)CCOC(=O)C1=C(Cc2ccccn2)c2ccccc2C1 10.1021/jm020895l
57326237 77154 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042407 77154 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
CHEMBL2078985 77154 0 None -2 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 326 5 0 2 3.3 C[N+](C)(C)C[C@@H]1COC[C@H](C(c2ccccc2)c2ccccc2)O1 10.1021/jm2013216
44337748 9363 0 None 1 2 Rat 5.1 pKi = 5.1 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
CHEMBL111529 9363 0 None 1 2 Rat 5.1 pKi = 5.1 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 183 1 0 3 1.0 CC(=O)O[C@H]1CC2CC(C1)N(C)C2 10.1021/jm00115a003
16125591 84669 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 455 6 2 2 3.8 C[N+]1(CC(=O)Nc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
CHEMBL222634 84669 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHOK1 cells
ChEMBL 455 6 2 2 3.8 C[N+]1(CC(=O)Nc2ccccc2)CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)C1 10.1021/jm061160+
90666118 109325 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 702 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CC[C@@H](OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
CHEMBL3219051 109325 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptorDisplacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
ChEMBL 702 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CC[C@@H](OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
44337761 9158 0 None -3 2 Rat 8.0 pKi = 8.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
CHEMBL110339 9158 0 None -3 2 Rat 8.0 pKi = 8.0 Binding
Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligandBinding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
ChEMBL 349 4 0 3 4.0 CN1CC2CC1C[C@H](OC(=O)C(C)(c1ccccc1)c1ccccc1)C2 10.1021/jm00115a003
44443731 94183 0 None 36 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 404 7 2 3 3.4 O=C(N[C@H]1[C@@H]2CN(CCc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL249830 94183 0 None 36 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 404 7 2 3 3.4 O=C(N[C@H]1[C@@H]2CN(CCc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
44627860 14003 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL1197371 14003 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
CHEMBL568870 14003 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 354 4 1 2 5.0 C[N+]1(C)CCC[C@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1 10.1021/jm901048j
53326934 58490 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 422 11 1 3 7.1 CCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683917 58490 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 422 11 1 3 7.1 CCCCCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
44308900 203973 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 367 5 2 4 1.4 NCCN1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL69582 203973 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 367 5 2 4 1.4 NCCN1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
277 1289 62 None -11 46 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1289 62 None -11 46 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1289 62 None -11 46 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1289 62 None -11 46 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1289 62 None -11 46 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
59291578 112758 0 None -1 3 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 313 3 1 5 3.0 O=C(Nc1ncoc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3298594 112758 0 None -1 3 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 313 3 1 5 3.0 O=C(Nc1ncoc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
CHEMBL3305763 112758 0 None -1 3 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
ChEMBL 313 3 1 5 3.0 O=C(Nc1ncoc1-c1ccccc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmc.2014.04.031
214124 169667 2 None -2 4 Human 8.0 pKi = 8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Muscarinic acetylcholine receptor M3 subtype
ChEMBL 331 8 0 3 4.4 CCN(CC)CCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
CHEMBL443780 169667 2 None -2 4 Human 8.0 pKi = 8 Binding
Antimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Muscarinic acetylcholine receptor M3 subtypeAntimuscarinic potency and subset specificity was characterised by its inhibition of the [3H]NMS Muscarinic acetylcholine receptor M3 subtype
ChEMBL 331 8 0 3 4.4 CCN(CC)CCOC(=O)C(C)(c1ccccc1)C1CCCCC1 10.1021/jm00085a017
135409468 2022 69 None -32 40 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
333 2022 69 None -32 40 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
CHEMBL845 2022 69 None -32 40 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
155515662 169940 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 336 4 0 3 3.9 O=C(OCc1ccccc1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
CHEMBL4441786 169940 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
ChEMBL 336 4 0 3 3.9 O=C(OCc1ccccc1)N(c1ccccc1)C1CN2CCC1CC2 10.1016/j.bmcl.2018.12.022
10862395 4994 0 None -22 5 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 406 4 1 5 4.4 CCOC(=O)c1c(CC)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL105148 4994 0 None -22 5 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 406 4 1 5 4.4 CCOC(=O)c1c(CC)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
11004046 5422 0 None -60 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 406 3 0 6 4.1 CCOC(=O)c1c(C)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
CHEMBL107444 5422 0 None -60 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
ChEMBL 406 3 0 6 4.1 CCOC(=O)c1c(C)n(C)c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3 10.1021/jm011116o
2551 791 23 None -54 11 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
11057 176125 23 None -2 20 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
3468 176125 23 None -2 20 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 176125 23 None -2 20 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL64894 176125 23 None -2 20 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
71716224 86927 0 None 1 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 317 4 0 5 1.9 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)Cc3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323444 86927 0 None 1 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 317 4 0 5 1.9 CC(=O)O[C@H]1C[C@@H]2C[C@@H](OC(=O)Cc3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
130442480 175246 0 None -112 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 175246 0 None -112 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-QNB/[3H]-NMS from human muscarinic M3 receptor expressed in stable CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
16125443 84620 0 None 3 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 335 3 1 2 3.1 CN1CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061159a
CHEMBL222402 84620 0 None 3 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cellsDisplacement of [3H]N-methyl-scopolamine from human muscarinic M3 receptor expressed in CHO K1 cells
ChEMBL 335 3 1 2 3.1 CN1CCC(N2CC(c3ccccc3)(c3ccccc3)NC2=O)CC1 10.1021/jm061159a
44308818 102054 0 None 2 3 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 360 5 3 3 3.4 NCc1cccc(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)c1 10.1016/s0960-894x(03)00350-0
CHEMBL302145 102054 0 None 2 3 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 360 5 3 3 3.4 NCc1cccc(NC(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)c1 10.1016/s0960-894x(03)00350-0
10598540 38299 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 426 6 2 3 5.0 O=C(NC1CCN(CC2CCCCCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
CHEMBL146291 38299 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cellsInhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
ChEMBL 426 6 2 3 5.0 O=C(NC1CCN(CC2CCCCCCC2)CC1)C(O)(c1ccccc1)C1CCCC1 10.1021/jm0003135
324 1912 15 None -17 9 Human 7.0 pKi = 7.0 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(01)00186-x
6436265 1912 15 None -17 9 Human 7.0 pKi = 7.0 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(01)00186-x
CHEMBL277642 1912 15 None -17 9 Human 7.0 pKi = 7.0 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(01)00186-x
324 1912 15 None -17 9 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
6436265 1912 15 None -17 9 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
CHEMBL277642 1912 15 None -17 9 Human 7.0 pKi = 7.0 Binding
Binding affinity against human muscarine receptor (hM3) cloned in CHO cellsBinding affinity against human muscarine receptor (hM3) cloned in CHO cells
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(02)00315-3
118719920 115747 0 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 509 10 0 7 4.5 CN1CCC=C(c2nsnc2OCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354066 115747 0 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assayDisplacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
ChEMBL 509 10 0 7 4.5 CN1CCC=C(c2nsnc2OCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
44308799 204006 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 6 1 3 3.5 CN(C)CCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
CHEMBL69765 204006 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cellsBinding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
ChEMBL 394 6 1 3 3.5 CN(C)CCC1CCN(C(=O)[C@](O)(c2ccccc2)[C@@H]2CCC(F)(F)C2)CC1 10.1016/s0960-894x(03)00350-0
164614994 188478 0 None -776 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 930 23 9 12 0.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4850553 188478 0 None -776 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 930 23 9 12 0.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028287 188478 0 None -776 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 930 23 9 12 0.9 CC(=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NCCN1CCN(C(=O)CCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
124087 1377 114 None -9 15 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1377 114 None -9 15 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1377 114 None -9 15 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1377 114 None -9 15 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1377 114 None -9 15 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
10660 14384 58 None -2 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
CHEMBL1200406 14384 58 None -2 12 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O nan
11759212 57862 0 None -117 6 Human 7.0 pKi = 7.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
CHEMBL167223 57862 0 None -117 6 Human 7.0 pKi = 7.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 326 5 0 2 4.8 CC(C1=C(CCN(C)C)Cc2cc(Cl)ccc21)c1ccccn1 10.1021/jm020895l
44627739 198349 0 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 333 4 1 3 4.3 CN1CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
CHEMBL576663 198349 0 None -3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M3 receptor expressed in CHO cells by scintillation counting
ChEMBL 333 4 1 3 4.3 CN1CCCC1c1ccc(C(O)(c2ccccc2)c2ccccc2)o1 10.1021/jm901048j
611066 157485 1 None -3 3 Rat 5.0 pKi = 5.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 381 4 2 6 0.9 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCO)CC2)c2ccccc21 10.1021/jm00111a032
CHEMBL407975 157485 1 None -3 3 Rat 5.0 pKi = 5.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 381 4 2 6 0.9 O=C1Nc2cccnc2N(C(=O)CN2CCN(CCO)CC2)c2ccccc21 10.1021/jm00111a032
71716225 86928 0 None -1 2 Rat 4.0 pKi = 4.0 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 317 4 0 5 1.9 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)Cc3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
CHEMBL2323445 86928 0 None -1 2 Rat 4.0 pKi = 4.0 Binding
Displacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 minsDisplacement of [3H]NMS from muscarinic M3 receptor in Sprague-Dawley rat submandibulary gland after 60 mins
ChEMBL 317 4 0 5 1.9 CC(=O)O[C@@H]1C[C@@H]2C[C@H](OC(=O)Cc3ccccc3)C[C@@H]1N2C 10.1016/j.bmc.2012.12.052
11834199 58741 0 None -21 5 Human 6.0 pKi = 6.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 7 0 2 4.9 CCN(CC)CCC1=C(C(C)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
CHEMBL168704 58741 0 None -21 5 Human 6.0 pKi = 6.0 Binding
Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamineBinding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
ChEMBL 320 7 0 2 4.9 CCN(CC)CCC1=C(C(C)c2ccccn2)c2ccccc2C1 10.1021/jm020895l
155513986 176463 0 None -562 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 760 19 10 8 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4439675 176463 0 None -562 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 760 19 10 8 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
CHEMBL4596667 176463 0 None -562 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting methodDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO-K9 cells after 3 hrs by microbeta2 scintillation counting method
ChEMBL 760 19 10 8 1.4 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCCCCC1CCN(CC(=O)N2c3ccccc3NC(=O)c3ccccc32)CC1 10.1021/acs.jmedchem.8b01967
154734599 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
327 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
4108 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
CHEMBL27673 2486 12 None -66 12 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm981038d
164620270 188518 0 None -8128 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL4869723 188518 0 None -8128 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
CHEMBL5028587 188518 0 None -8128 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from human muscarinic M3 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 903 21 10 13 -1.3 CC(=O)N[C@@H](CCCN)C(=O)NC(=O)[C@H](C)NC(=O)[C@H](CCNC(=N)N)NCCN1CCN(CCC(=O)NC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)CC1 10.1016/j.ejmech.2021.113159
162670602 182913 0 None -1 2 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 248 2 0 2 1.8 O=C(CN1CCc2ccc(F)cc21)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4792675 182913 0 None -1 2 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 248 2 0 2 1.8 O=C(CN1CCc2ccc(F)cc21)N1CCCC1 10.1016/j.bmcl.2020.127632
202119 12003 3 None -1 3 Rat 5.0 pKi = 5.0 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@H]1O[C@@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL1183388 12003 3 None -1 3 Rat 5.0 pKi = 5.0 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@H]1O[C@@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
CHEMBL294470 12003 3 None -1 3 Rat 5.0 pKi = 5.0 Binding
Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glandsBinding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
ChEMBL 172 2 0 2 0.4 C[C@H]1O[C@@H](C[N+](C)(C)C)CC1=O 10.1021/jm00088a029
44443721 94233 0 None 14 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 390 6 2 3 3.3 O=C(N[C@H]1[C@@H]2CN(Cc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
CHEMBL250203 94233 0 None 14 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
ChEMBL 390 6 2 3 3.3 O=C(N[C@H]1[C@@H]2CN(Cc3ccccc3)C[C@@H]21)C(O)(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.06.081
5353853 17954 47 None -13 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 17954 47 None -13 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 17954 47 None -13 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
44400218 67599 0 None 2 2 Rat 6.0 pKi = 6.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 383 6 1 5 2.6 COc1ccc(C(O)(C(=O)OCC#CCN2CC3CC3C2)C2CCCC2)cc1 10.1016/j.bmcl.2005.02.036
CHEMBL190459 67599 0 None 2 2 Rat 6.0 pKi = 6.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
ChEMBL 383 6 1 5 2.6 COc1ccc(C(O)(C(=O)OCC#CCN2CC3CC3C2)C2CCCC2)cc1 10.1016/j.bmcl.2005.02.036
10865439 20593 0 None -10 5 Human 7.0 pKi = 7.0 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 715 15 0 6 7.6 COc1ccccc1CN1CCC(C2CCN(C(=O)CCCCCCC(=O)N3CCC(C4CCN(Cc5ccccc5OC)CC4)CC3)CC2)CC1 10.1021/jm0155594
CHEMBL130835 20593 0 None -10 5 Human 7.0 pKi = 7.0 Binding
Affinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cellsAffinity for human M3 cloned muscarinic receptor subtype expressed in CHO-K1 cells
ChEMBL 715 15 0 6 7.6 COc1ccccc1CN1CCC(C2CCN(C(=O)CCCCCCC(=O)N3CCC(C4CCN(Cc5ccccc5OC)CC4)CC3)CC2)CC1 10.1021/jm0155594
135466875 189091 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 769 25 5 10 6.6 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
CHEMBL510340 189091 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in insect Sf9 cells
ChEMBL 769 25 5 10 6.6 CCCCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCNC1=O 10.1021/np050091j
15050950 204034 0 None -1 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 422 5 2 6 1.1 CC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
CHEMBL70003 204034 0 None -1 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
ChEMBL 422 5 2 6 1.1 CC(=O)NCCN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1 10.1021/jm00111a032
109014373 179778 1 None -10 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.1 CC1CCN(C(=O)CCN2CCCc3ccccc32)CC1 10.1016/j.bmcl.2020.127632
CHEMBL4744856 179778 1 None -10 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysisDisplacement of [3H]-NMS from muscarinic M3 receptor (unknown origin) expressed in CHO-K1 cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL 286 3 0 2 3.1 CC1CCN(C(=O)CCN2CCCc3ccccc32)CC1 10.1016/j.bmcl.2020.127632
156011112 178251 0 None -4 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4633679 178251 0 None -4 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
CHEMBL4650842 178251 0 None -4 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M3 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Sc3ccccc3)cc2)CO1 10.1021/acs.jmedchem.9b02100
10418420 70244 0 None -74 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 955 27 0 10 10.9 CN(CCCCCCCCN(C)CCCCCCN1CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2)CCCCCCN1CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00113-8
CHEMBL194216 70244 0 None -74 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenatesInhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
ChEMBL 955 27 0 10 10.9 CN(CCCCCCCCN(C)CCCCCCN1CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2)CCCCCCN1CCC2(CC1)OC(=O)C(c1ccccc1)(c1ccccc1)O2 10.1016/0960-894X(95)00113-8
57326144 77162 0 None -1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@H](c2ccccc2)O1 10.1021/jm2013216
CHEMBL2042402 77162 0 None -1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@H](c2ccccc2)O1 10.1021/jm2013216
CHEMBL2079061 77162 0 None -1 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 236 3 0 2 1.8 C[N+](C)(C)C[C@@H]1COC[C@H](c2ccccc2)O1 10.1021/jm2013216
44274477 165544 0 None -3 5 Human 4.0 pKi = 4.0 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 331 2 0 3 2.8 CN1CCN(C(=O)C2=C/C(=C\c3ccncc3)c3ccccc32)CC1 10.1016/s0960-894x(01)00186-x
CHEMBL424214 165544 0 None -3 5 Human 4.0 pKi = 4.0 Binding
Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
ChEMBL 331 2 0 3 2.8 CN1CCN(C(=O)C2=C/C(=C\c3ccncc3)c3ccccc32)CC1 10.1016/s0960-894x(01)00186-x
53326849 58497 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 381 8 2 4 4.5 NCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683923 58497 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assayDisplacement of [3H]-N-methyl-scopolamine from human muscarinic M3 receptor after 6 hrs by cell based assay
ChEMBL 381 8 2 4 4.5 NCCCCCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1016/j.bmcl.2011.01.043
657255 199061 34 None -11 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
CHEMBL588119 199061 34 None -11 15 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 nan
10984804 98448 0 None 30 2 Human 7.0 pKi = 7 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NC[C@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
CHEMBL275914 98448 0 None 30 2 Human 7.0 pKi = 7 Binding
Inhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cellsInhibition of [3H]NMS binding to human cloned M3 receptor expressed in CHO cells
ChEMBL 592 9 2 4 4.5 O=C(NC[C@H]1CCCNC1)[C@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CC(c1ccccc1)(c1ccccc1)c1ccccc1 10.1021/jm051205r
2551 791 23 None -54 11 Rat 6.0 pKi = 6 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 791 23 None -54 11 Rat 6.0 pKi = 6 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 791 23 None -54 11 Rat 6.0 pKi = 6 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 791 23 None -54 11 Rat 6.0 pKi = 6 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 791 23 None -54 11 Rat 6.0 pKi = 6 Binding
Displacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cellsDisplacement of [3H]NMS from rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
154734599 2486 12 None -66 12 Rat 6.0 pKi = 6 Binding
Compound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary glandCompound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm970740r
327 2486 12 None -66 12 Rat 6.0 pKi = 6 Binding
Compound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary glandCompound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm970740r
4108 2486 12 None -66 12 Rat 6.0 pKi = 6 Binding
Compound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary glandCompound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm970740r
CHEMBL27673 2486 12 None -66 12 Rat 6.0 pKi = 6 Binding
Compound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary glandCompound was tested for its binding affinity towards Muscarinic acetylcholine receptor M3 using [3H]NMS from rat submaxillary gland
ChEMBL 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 10.1021/jm970740r
154059 3610 51 None -1 8 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
2457 3610 51 None -1 8 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
7483 3610 51 None -1 8 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
CHEMBL1734 3610 51 None -1 8 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
DB01591 3610 51 None -1 8 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation countingDisplacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
306 3430 21 None -4 5 Human 8.1 pIC50 = 8.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
3536 3430 21 None -4 5 Human 8.1 pIC50 = 8.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
53930639 3430 21 None -4 5 Human 8.1 pIC50 = 8.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
9577995 3430 21 None -4 5 Human 8.1 pIC50 = 8.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
CHEMBL134641 3430 21 None -4 5 Human 8.1 pIC50 = 8.1 Binding
In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3
Drug Central 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N None
2745 3832 42 None -21 9 Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3832 42 None -21 9 Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3832 42 None -21 9 Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3832 42 None -21 9 Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3832 42 None -21 9 Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3832 42 None -21 9 Human 8.1 pIC50 = 8.1 Binding
Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
Drug Central 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
2824 3962 0 None 1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
345 3962 0 None 1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
71203 3962 0 None 1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
CHEMBL1892145 3962 0 None 1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
DB13793 3962 0 None 1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 None
92112 21673 18 None -1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@@]12CCCN3CCc4c(n(c5ccccc45)C(=O)C1)[C@H]32 None
CHEMBL1318553 21673 18 None -1 4 Human 8.3 pKd = 8.3 Binding
NoneNone
Drug Central 294 1 0 3 3.8 CC[C@@]12CCCN3CCc4c(n(c5ccccc45)C(=O)C1)[C@H]32 None
2360 3667 43 None -1 5 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
2484 3667 43 None -1 5 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
347 3667 43 None -1 5 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
441071 3667 43 None -1 5 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
CHEMBL227934 3667 43 None -1 5 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
DB15954 3667 43 None -1 5 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 None
15376 3963 0 None 1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
349 3963 0 None 1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
3643 3963 0 None 1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
CHEMBL1165342 3963 0 None 1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
DB13374 3963 0 None 1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 None
21158560 112766 7 None -1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 666 6 2 4 5.5 C=CC[N@@+]12CC[C@@]34c5ccccc5N5/C=C6/[C@H]7C[C@H]8[C@@]9(CC[N@@+]8(CC=C)C/C7=C/CO)c7ccccc7N(/C=C(/[C@@H](C[C@@H]31)/C(=C\CO)C2)[C@H]54)[C@@H]69 None
CHEMBL3305985 112766 7 None -1 4 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 666 6 2 4 5.5 C=CC[N@@+]12CC[C@@]34c5ccccc5N5/C=C6/[C@H]7C[C@H]8[C@@]9(CC[N@@+]8(CC=C)C/C7=C/CO)c7ccccc7N(/C=C(/[C@@H](C[C@@H]31)/C(=C\CO)C2)[C@H]54)[C@@H]69 None
2381 660 48 None -9 9 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
374 660 48 None -9 9 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
7128 660 48 None -9 9 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
CHEMBL1101 660 48 None -9 9 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
DB00810 660 48 None -9 9 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
656598 12700 6 None -2 4 Rat 8.1 pKd = 8.1 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
Drug Central 304 4 1 3 2.1 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL1187724 12700 6 None -2 4 Rat 8.1 pKd = 8.1 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
Drug Central 304 4 1 3 2.1 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL516476 12700 6 None -2 4 Rat 8.1 pKd = 8.1 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
Drug Central 304 4 1 3 2.1 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
11968014 12726 5 None -1 9 Rat 8.0 pKd = 8.0 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
Drug Central 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 None
CHEMBL1187846 12726 5 None -1 9 Rat 8.0 pKd = 8.0 Binding
In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepineIn vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine
Drug Central 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 None
319 1312 44 None 2 9 Human 8.0 pKd = 8.0 Binding
GRAC: human M3 probeGRAC: human M3 probe
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
321 1312 44 None 2 9 Human 8.0 pKd = 8.0 Binding
GRAC: human M3 probeGRAC: human M3 probe
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
444031 1312 44 None 2 9 Human 8.0 pKd = 8.0 Binding
GRAC: human M3 probeGRAC: human M3 probe
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
784 1312 44 None 2 9 Human 8.0 pKd = 8.0 Binding
GRAC: human M3 probeGRAC: human M3 probe
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
CHEMBL1346 1312 44 None 2 9 Human 8.0 pKd = 8.0 Binding
GRAC: human M3 probeGRAC: human M3 probe
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
DB00496 1312 44 None 2 9 Human 8.0 pKd = 8.0 Binding
GRAC: human M3 probeGRAC: human M3 probe
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
12165 908 6 None -15 2 Human 10.2 pKd = 10.2 Binding
Binding to human cloned M3 receptor using [3H]-N-methylscopolamine as tracerBinding to human cloned M3 receptor using [3H]-N-methylscopolamine as tracer
Guide to Pharmacology 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 35901125
90200922 908 6 None -15 2 Human 10.2 pKd = 10.2 Binding
Binding to human cloned M3 receptor using [3H]-N-methylscopolamine as tracerBinding to human cloned M3 receptor using [3H]-N-methylscopolamine as tracer
Guide to Pharmacology 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 35901125
CHEMBL5172865 908 6 None -15 2 Human 10.2 pKd = 10.2 Binding
Binding to human cloned M3 receptor using [3H]-N-methylscopolamine as tracerBinding to human cloned M3 receptor using [3H]-N-methylscopolamine as tracer
Guide to Pharmacology 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 35901125
23056 112 29 None -1 8 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 3443095
23056 112 29 None -1 8 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
318 112 29 None -1 8 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 3443095
318 112 29 None -1 8 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
3260 112 29 None -1 8 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 3443095
3260 112 29 None -1 8 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
CHEMBL12980 112 29 None -1 8 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 3443095
CHEMBL12980 112 29 None -1 8 Human 10.4 pKd = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 7562472
367 3795 12 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
5487427 3795 12 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
8592 3795 12 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
CHEMBL1900528 3795 12 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
CHEMBL3305968 3795 12 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
CHEMBL4650755 3795 12 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
DB01409 3795 12 None 2 8 Human 10.7 pKd = 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 23435542
344 2729 0 None -19 5 Human 3.3 pKd = 3.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 3 0 4 2.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)CCl 9495826
44358908 2729 0 None -19 5 Human 3.3 pKd = 3.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 3 0 4 2.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)CCl 9495826
CHEMBL139677 2729 0 None -19 5 Human 3.3 pKd = 3.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 3 0 4 2.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)CCl 9495826
15118529 4052 0 None -6 4 Human 5.1 pKd = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 0 1 4 5.4 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CCC2=Cc3c(C[C@]12C)cn1c(n3)nc2c1cccc2 12435818
340 4052 0 None -6 4 Human 5.1 pKd = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 0 1 4 5.4 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CCC2=Cc3c(C[C@]12C)cn1c(n3)nc2c1cccc2 12435818
CHEMBL1256845 4052 0 None -6 4 Human 5.1 pKd = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 0 1 4 5.4 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CCC2=Cc3c(C[C@]12C)cn1c(n3)nc2c1cccc2 12435818
2381 660 48 None -9 9 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
374 660 48 None -9 9 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
7128 660 48 None -9 9 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
CHEMBL1101 660 48 None -9 9 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
DB00810 660 48 None -9 9 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 1346637
319 1312 44 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9029489
321 1312 44 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9029489
444031 1312 44 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9029489
784 1312 44 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9029489
CHEMBL1346 1312 44 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9029489
DB00496 1312 44 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9029489
316 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 11303071
316 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
316 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
316 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
316 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
316 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
317 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 11303071
317 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
317 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
317 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
317 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
317 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
71183 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 11303071
71183 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
71183 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
71183 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
71183 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
71183 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
CHEMBL3140030 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 11303071
CHEMBL3140030 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
CHEMBL3140030 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
CHEMBL3140030 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
CHEMBL3140030 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
CHEMBL3140030 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
CHEMBL376897 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 11303071
CHEMBL376897 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
CHEMBL376897 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
CHEMBL376897 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
CHEMBL376897 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
CHEMBL376897 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
DB00462 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 11303071
DB00462 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16369696
DB00462 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7562472
DB00462 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7651370
DB00462 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9224827
DB00462 2816 19 None -2 9 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 9846649
316 2816 19 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 12235229
316 2816 19 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
317 2816 19 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 12235229
317 2816 19 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
71183 2816 19 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 12235229
71183 2816 19 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
CHEMBL3140030 2816 19 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 12235229
CHEMBL3140030 2816 19 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
CHEMBL376897 2816 19 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 12235229
CHEMBL376897 2816 19 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
DB00462 2816 19 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 12235229
DB00462 2816 19 None 1 9 Rat 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 7687290
21123938 730 0 None -12 5 Human 2.5 pKd None 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N@@+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)[O-] 9495826
343 730 0 None -12 5 Human 2.5 pKd None 2.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N@@+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)[O-] 9495826
342 729 55 None -35 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9224827
342 729 55 None -35 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9495826
442021 729 55 None -35 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9224827
442021 729 55 None -35 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9495826
CHEMBL501756 729 55 None -35 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9224827
CHEMBL501756 729 55 None -35 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 2 0 5 2.1 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CCN2[C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2 9495826
332 2021 0 None -10 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 4 3.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)Cc1ccccc1 9495826
44358893 2021 0 None -10 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 4 3.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)Cc1ccccc1 9495826
CHEMBL343796 2021 0 None -10 5 Human 3.8 pKd None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 4 3.8 COc1cc2c(cc1OC)N1[C@@H]3[C@@]42CC[N+]2([C@H]4C[C@@H]4[C@H]3[C@H](CC1=O)OCC=C4C2)Cc1ccccc1 9495826
348 3774 0 None 1 4 Human 4.4 pKd None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 2 1 6 1.9 OCCc1sc2=Nc3c(Cn2c1C)cnc(n3)C 14722259
66706 3774 0 None 1 4 Human 4.4 pKd None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 2 1 6 1.9 OCCc1sc2=Nc3c(Cn2c1C)cnc(n3)C 14722259
2360 3667 43 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
2360 3667 43 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
2484 3667 43 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
2484 3667 43 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
347 3667 43 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
347 3667 43 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
441071 3667 43 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
441071 3667 43 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
CHEMBL227934 3667 43 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
CHEMBL227934 3667 43 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
DB15954 3667 43 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 7651370
DB15954 3667 43 None -1 5 Human 5.0 pKd None 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 0 0 3 2.1 O=C1C[C@@H]2OCC=C3[C@H]4[C@@H]2[C@@H]2N1c1ccccc1[C@]12CCN([C@H]1C4)C3 9224827
335 1823 0 None -5 4 Human 5.1 pKd None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 470 5 2 7 3.3 COc1ccc2c(c1)c1c3c(=O)[nH]c(=O)c3c3c(c1n2CC(CN(C)C)O)n(C)c1c3cccc1 10860942
3500 1823 0 None -5 4 Human 5.1 pKd None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 470 5 2 7 3.3 COc1ccc2c(c1)c1c3c(=O)[nH]c(=O)c3c3c(c1n2CC(CN(C)C)O)n(C)c1c3cccc1 10860942
CHEMBL157822 1823 0 None -5 4 Human 5.1 pKd None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 470 5 2 7 3.3 COc1ccc2c(c1)c1c3c(=O)[nH]c(=O)c3c3c(c1n2CC(CN(C)C)O)n(C)c1c3cccc1 10860942
2824 3962 0 None 1 4 Human 5.2 pKd None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
345 3962 0 None 1 4 Human 5.2 pKd None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
71203 3962 0 None 1 4 Human 5.2 pKd None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
CHEMBL1892145 3962 0 None 1 4 Human 5.2 pKd None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
DB13793 3962 0 None 1 4 Human 5.2 pKd None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 1 0 3 3.8 CC[C@]12CCCN3[C@@H]2c2n(C(=O)C1)c1c(c2CC3)cccc1 9224827
339 4050 0 None -5 4 Human 5.5 pKd None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 0 1 4 5.2 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CC[C@@H]2[C@]1(C)Cc1cn3c(nc1C2)nc1c3cccc1 12435818
9803245 4050 0 None -5 4 Human 5.5 pKd None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 0 1 4 5.2 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CC[C@@H]2[C@]1(C)Cc1cn3c(nc1C2)nc1c3cccc1 12435818
CHEMBL2206331 4050 0 None -5 4 Human 5.5 pKd None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 0 1 4 5.2 C#C[C@]1(O)CC[C@@H]2[C@]1(C)CC[C@H]1[C@H]2CC[C@@H]2[C@]1(C)Cc1cn3c(nc1C2)nc1c3cccc1 12435818
15376 3963 0 None 1 4 Human 5.7 pKd None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
349 3963 0 None 1 4 Human 5.7 pKd None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
3643 3963 0 None 1 4 Human 5.7 pKd None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
CHEMBL1165342 3963 0 None 1 4 Human 5.7 pKd None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
DB13374 3963 0 None 1 4 Human 5.7 pKd None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 2 1 5 3.0 COC(=O)[C@@]1(O)C[C@]2(CC)CCCN3[C@@H]2c2n1c1ccccc1c2CC3 9224827
341 339 0 None -5 4 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 666 6 2 4 5.5 C=CC[N+]12CC[C@@]34[C@@H]2C[C@@H](C(=CCO)C1)C1=CN2c5ccccc5[C@]56[C@@H]2C(=CN([C@H]31)c1c4cccc1)[C@H]1C[C@@H]6[N+](CC1=CCO)(CC5)CC=C 9224827
5311001 339 0 None -5 4 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 666 6 2 4 5.5 C=CC[N+]12CC[C@@]34[C@@H]2C[C@@H](C(=CCO)C1)C1=CN2c5ccccc5[C@]56[C@@H]2C(=CN([C@H]31)c1c4cccc1)[C@H]1C[C@@H]6[N+](CC1=CCO)(CC5)CC=C 9224827
23056 112 29 3H-QNB -1 8 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
318 112 29 3H-QNB -1 8 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
3260 112 29 3H-QNB -1 8 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
CHEMBL12980 112 29 3H-QNB -1 8 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
23056 112 29 3H-QNB -1 8 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
318 112 29 3H-QNB -1 8 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
3260 112 29 3H-QNB -1 8 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
CHEMBL12980 112 29 3H-QNB -1 8 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 337 4 1 4 2.6 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CN2CCC1CC2 None
12057539 208018 42 3H-Arachidonic Acid 1 21 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 3H-Arachidonic Acid 1 21 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 3H-Arachidonic Acid 1 21 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
12057539 208018 42 3H-NMS 1 21 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 3H-NMS 1 21 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 3H-NMS 1 21 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
131632304 216011 0 3H-NMS -1 13 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
12057539 208018 42 3H-QNB 1 21 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 3H-QNB 1 21 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 3H-QNB 1 21 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
44431393 87995 0 UNDEFINED -1 3 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 402 6 1 5 3.5 CN(C)C1(CNCCC2CCOCC2)COc2cc(Cl)c(Cl)cc2OC1 None
CHEMBL234440 87995 0 UNDEFINED -1 3 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 402 6 1 5 3.5 CN(C)C1(CNCCC2CCOCC2)COc2cc(Cl)c(Cl)cc2OC1 None
12057539 208018 42 3H-NMS -2 21 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 3H-NMS -2 21 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 3H-NMS -2 21 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
325 2049 0 3H-NMS -1 9 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
3746 2049 0 3H-NMS -1 9 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
657308 2049 0 3H-NMS -1 9 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
CHEMBL1615433 2049 0 3H-NMS -1 9 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
DB00332 2049 0 3H-NMS -1 9 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
12057539 208018 42 3H-PIRENZEPINE -2 21 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 3H-PIRENZEPINE -2 21 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 3H-PIRENZEPINE -2 21 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
131632304 216011 0 3H-QNB -3 13 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
1734 116 10 3H-4-DAMP 1 13 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 10 3H-4-DAMP 1 13 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 10 3H-4-DAMP 1 13 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
12057539 208018 42 3H-NMS 1 21 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 3H-NMS 1 21 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 3H-NMS 1 21 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
325 2049 0 3H-NMS -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
3746 2049 0 3H-NMS -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
657308 2049 0 3H-NMS -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
CHEMBL1615433 2049 0 3H-NMS -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
DB00332 2049 0 3H-NMS -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C None
1734 116 10 3H-NMS 1 13 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 10 3H-NMS 1 13 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 10 3H-NMS 1 13 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
1734 116 10 3H-NMS -2 13 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 10 3H-NMS -2 13 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 10 3H-NMS -2 13 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
2028 2958 80 3H-NMS -1 11 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
359 2958 80 3H-NMS -1 11 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634 2958 80 3H-NMS -1 11 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
CHEMBL1231 2958 80 3H-NMS -1 11 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
DB01062 2958 80 3H-NMS -1 11 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
1734 116 10 3H-QNB 1 13 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 10 3H-QNB 1 13 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 10 3H-QNB 1 13 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
3246155 215937 0 3H-NMS -3 17 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 307 4 0 2 4.4 CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 None
2028 2958 80 UNDEFINED 1 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
359 2958 80 UNDEFINED 1 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634 2958 80 UNDEFINED 1 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
CHEMBL1231 2958 80 UNDEFINED 1 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
DB01062 2958 80 UNDEFINED 1 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
12057539 208018 42 3H-NMS 1 21 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
12057539 208018 42 3H-NMSP 1 21 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 3H-NMS 1 21 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 3H-NMSP 1 21 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 3H-NMS 1 21 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 3H-NMSP 1 21 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
None 216202 0 3H-NMS 1 6 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 426 7 1 3 4.0 C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5 None
1734 116 10 3H-PIRENZEPINE -2 13 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 10 3H-PIRENZEPINE -2 13 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 10 3H-PIRENZEPINE -2 13 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
12057539 208018 42 3H-NMS -2 21 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 3H-NMS -2 21 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 3H-NMS -2 21 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
12057539 208018 42 3H-QNB 1 21 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 3H-QNB 1 21 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 3H-QNB 1 21 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3246155 215937 0 3H-QNB -4 17 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 307 4 0 2 4.4 CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 None
130169 3578 0 3H-NMS 1 5 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O None
331 3578 0 3H-NMS 1 5 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O None
None 216202 0 3H-NMS -1 6 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 426 7 1 3 4.0 C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5 None
44431384 148836 0 UNDEFINED -2 3 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 384 6 1 4 4.0 CN(C)C1(CNCCC23CC4CC(CC(C4)C2)C3)COc2ccccc2OC1 None
CHEMBL394137 148836 0 UNDEFINED -2 3 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 384 6 1 4 4.0 CN(C)C1(CNCCC23CC4CC(CC(C4)C2)C3)COc2ccccc2OC1 None
3042 1402 35 3H-NMS 1 15 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 1402 35 3H-NMS 1 15 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 1402 35 3H-NMS 1 15 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 1402 35 3H-NMS 1 15 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 1402 35 3H-NMS 1 15 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
2381 660 48 3H-NMS -3 9 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
374 660 48 3H-NMS -3 9 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
7128 660 48 3H-NMS -3 9 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
CHEMBL1101 660 48 3H-NMS -3 9 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
DB00810 660 48 3H-NMS -3 9 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
2293 3164 27 None -1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
329 3164 27 None -1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
4934 3164 27 None -1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
CHEMBL1180725 3164 27 None -1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
DB00782 3164 27 None -1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C None
310 1909 0 3H-NMS -3 11 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
3602 1909 0 3H-NMS -3 11 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
CHEMBL3545990 1909 0 3H-NMS -3 11 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
11434515 261 6 None -4 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
11519741 261 6 None -4 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
4484 261 6 None -4 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
7449 261 6 None -4 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
CHEMBL1194325 261 6 None -4 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
DB08897 261 6 None -4 5 Human 8.0 pKi = 8.0 Binding
Binding affinity to muscarinic M3 receptorBinding affinity to muscarinic M3 receptor
Drug Central 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 None
11519069 3908 3 None 1 5 Human 8.0 pKi = 8.0 Binding
radioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligandradioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligand
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
11519070 3908 3 None 1 5 Human 8.0 pKi = 8.0 Binding
radioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligandradioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligand
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
4816 3908 3 None 1 5 Human 8.0 pKi = 8.0 Binding
radioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligandradioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligand
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
7354 3908 3 None 1 5 Human 8.0 pKi = 8.0 Binding
radioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligandradioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligand
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
CHEMBL1187833 3908 3 None 1 5 Human 8.0 pKi = 8.0 Binding
radioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligandradioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligand
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
DB09076 3908 3 None 1 5 Human 8.0 pKi = 8.0 Binding
radioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligandradioligand binding assays in CHO cells expressing human M1, M2, or M3 receptors in a scintillation proximity assay with 0.5 nM [3H]-N-methyl scopolamine as the ligand
Drug Central 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 None
316 2816 19 None -2 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
317 2816 19 None -2 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
71183 2816 19 None -2 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL3140030 2816 19 None -2 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL376897 2816 19 None -2 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
DB00462 2816 19 None -2 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
154825138 216012 0 3H-4-DAMP -17 12 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
1209 1645 75 3H-QNB -30 32 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1645 75 3H-QNB -30 32 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1645 75 3H-QNB -30 32 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1645 75 3H-QNB -30 32 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1645 75 3H-QNB -30 32 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
214 3831 58 3H-QNB -1202 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3831 58 3H-QNB -1202 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3831 58 3H-QNB -1202 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3831 58 3H-QNB -1202 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3831 58 3H-QNB -1202 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3831 58 3H-QNB -1202 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
46222048 8952 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
CHEMBL1098230 8952 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
11957621 216013 0 3H-NMS -12 10 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 203 3 2 3 1.3 COC1=C(C=CC(=C1)CCN)O.Cl None
11957621 216013 0 3H-NMS -12 10 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 203 3 2 3 1.3 COC1=C(C=CC(=C1)CCN)O.Cl None
3075702 217305 0 3H-4-DAMP -2 37 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
145 140 49 3H-QNB -1949 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 49 3H-QNB -1949 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 49 3H-QNB -1949 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 49 3H-QNB -1949 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
179 399 115 3H-QNB -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 399 115 3H-QNB -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 399 115 3H-QNB -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 399 115 3H-QNB -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 399 115 3H-QNB -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
141 1415 35 3H-QNB -114 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1415 35 3H-QNB -114 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1415 35 3H-QNB -114 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1415 35 3H-QNB -114 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
119376 1828 48 3H-DAMP -54954 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 1828 48 3H-DAMP -54954 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 1828 48 3H-DAMP -54954 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
1353 1898 93 3H-QNB -154 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1898 93 3H-QNB -154 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1898 93 3H-QNB -154 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1898 93 3H-QNB -154 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1898 93 3H-QNB -154 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3294 1993 111 3H-NMS -14454 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1993 111 3H-NMS -14454 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1993 111 3H-NMS -14454 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1993 111 3H-NMS -14454 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1993 111 3H-NMS -14454 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1588 2311 27 3H-QNB -28840 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2311 27 3H-QNB -28840 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2311 27 3H-QNB -28840 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2311 27 3H-QNB -28840 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2311 27 3H-QNB -28840 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1830 2572 44 3H-QNB -39 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1830 2572 44 3H-QNB -1778 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2572 44 3H-QNB -39 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2572 44 3H-QNB -1778 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2572 44 3H-QNB -39 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2572 44 3H-QNB -1778 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2572 44 3H-QNB -39 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2572 44 3H-QNB -1778 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2572 44 3H-QNB -39 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2572 44 3H-QNB -1778 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
15897 2840 0 3H-QNB -32 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2840 0 3H-QNB -32 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2840 0 3H-QNB -32 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
119570 3137 96 3H-QNB -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3137 96 3H-QNB -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3137 96 3H-QNB -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3137 96 3H-QNB -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3137 96 3H-QNB -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2337 3232 77 3H-QNB -81 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3232 77 3H-QNB -81 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3232 77 3H-QNB -81 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3232 77 3H-QNB -81 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3232 77 3H-QNB -81 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2389 3306 118 3H-QNB -602 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3306 118 3H-QNB -602 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3306 118 3H-QNB -602 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3306 118 3H-QNB -602 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3306 118 3H-QNB -602 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
128563 3438 33 3H-QNB -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3438 33 3H-QNB -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3438 33 3H-QNB -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3438 33 3H-QNB -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1267 3775 49 3H-NMS -4168 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3775 49 3H-NMS -4168 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3775 49 3H-NMS -4168 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
213 3824 55 3H-QNB -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3824 55 3H-QNB -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3824 55 3H-QNB -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3824 55 3H-QNB -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3824 55 3H-QNB -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
185 3975 60 3H-QNB -30902 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3975 60 3H-QNB -30902 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3975 60 3H-QNB -30902 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3975 60 3H-QNB -30902 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
2865 4112 73 3H-QNB -812 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4112 73 3H-QNB -812 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4112 73 3H-QNB -812 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4112 73 3H-QNB -812 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4112 73 3H-QNB -812 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
103 4122 61 3H-QNB -144 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4122 61 3H-QNB -144 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4122 61 3H-QNB -144 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4122 61 3H-QNB -144 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4122 61 3H-QNB -144 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
10297 27081 30 3H-QNB -38 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 27081 30 3H-QNB -38 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
15387 45792 55 3H-QNB -1479 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45792 55 3H-QNB -1479 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
115237 55555 119 3H-QNB -42657 55 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55555 119 3H-QNB -42657 55 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1979 77297 70 3H-cAMP 2 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
CHEMBL20835 77297 70 3H-cAMP 2 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
3025067 99354 64 3H-NMS -512 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
65853 99354 64 3H-NMS -512 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
CHEMBL282614 99354 64 3H-NMS -512 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
3663 99939 83 3H-QNB -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 99939 83 3H-QNB -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
37632 111565 28 3H-QNB -1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 0 5 3.3 CN(C)Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 None
CHEMBL328250 111565 28 3H-QNB -1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 0 5 3.3 CN(C)Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 None
3452843 119499 15 3H-NMS -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 None
CHEMBL345686 119499 15 3H-NMS -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 None
446220 133496 14 3H-QNB -1778 46 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 133496 14 3H-QNB -1778 46 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
5280343 188251 124 3H-QNB -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 188251 124 3H-QNB -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 188251 124 3H-QNB -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
162265 202251 22 3H-QNB -239 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202251 22 3H-QNB -239 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202251 22 3H-QNB -239 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
5281600 203002 92 3H-QNB -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 203002 92 3H-QNB -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
5656 203043 87 3H-QNB -79 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 203043 87 3H-QNB -79 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
1973 203460 15 3H-4-DAMP -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 203460 15 3H-4-DAMP -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 203460 15 3H-4-DAMP -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
202478 204664 20 3H-QNB -97 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 204664 20 3H-QNB -97 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
5311189 204818 11 3H-QNB -194 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 204818 11 3H-QNB -194 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
4158 205318 21 3H-QNB -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 205318 21 3H-QNB -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 205318 21 3H-QNB -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
4054 205478 72 3H-QNB -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 205478 72 3H-QNB -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 205478 72 3H-QNB -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
3337 206344 27 3H-QNB -158 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-QNB -158 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-QNB -158 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-QNB -158 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-QNB -158 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
444 206643 53 3H-QNB -2089 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 3 1 2 3.3 CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1 None
CHEMBL894 206643 53 3H-QNB -2089 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 3 1 2 3.3 CC(NC(C)(C)C)C(=O)c1cccc(Cl)c1 None
16231 207486 57 3H-NMS -7 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
CHEMBL945 207486 57 3H-NMS -7 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
11954224 215928 0 3H-QNB -141253 60 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
5831 215938 0 3H-NMS -51 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
5831 215938 0 3H-NMS -2344 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
11954259 215954 0 3H-QNB -13182 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
40589 216118 0 3H-QNB -407 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 377 7 0 6 2.5 CCC1=NN(C(=O)N1CC)CCCN2CCN(CC2)C3=CC(=CC=C3)Cl None
25137849 216153 0 3H-QNB -4 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 216153 0 3H-QNB -4 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 216213 0 3H-QNB -38018 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
None 216280 0 3H-NMS 1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 483 7 3 4 4.4 CC(CCC(=O)NCCS(=O)(=O)O)C1CCC2C1(CCC3C2CCC4C3(CCC(C4)O)C)C None
None 216280 0 3H-NMS -1 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 483 7 3 4 4.4 CC(CCC(=O)NCCS(=O)(=O)O)C1CCC2C1(CCC3C2CCC4C3(CCC(C4)O)C)C None
None 216281 0 3H-NMS 1 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 433 6 3 3 4.6 CC(CCC(=O)NCC(=O)O)C1CCC2C1(CCC3C2CCC4C3(CCC(C4)O)C)C None
None 216281 0 3H-NMS -1 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 433 6 3 3 4.6 CC(CCC(=O)NCC(=O)O)C1CCC2C1(CCC3C2CCC4C3(CCC(C4)O)C)C None
None 216285 0 3H-QNB -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 216286 0 3H-QNB -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 216287 0 3H-QNB -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 216288 0 3H-QNB -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 216289 0 3H-QNB -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 216290 0 3H-QNB -1 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 216291 0 3H-QNB -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 216292 0 3H-QNB -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 216299 0 3H-QNB -13 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 216300 0 3H-QNB -16 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 216301 0 3H-QNB -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
4978 216302 0 3H-QNB -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 216303 0 3H-QNB -3 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 216304 0 3H-QNB -281 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 216305 0 3H-QNB -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
None 216423 0 UNDEFINED -660 28 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 216467 0 3H-NMS -1 14 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 399 7 4 5 1.8 CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O.C(CC(=O)O)C(=O)O.O None
214 3831 58 3H-QNB -93 30 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3831 58 3H-QNB -93 30 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3831 58 3H-QNB -93 30 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3831 58 3H-QNB -93 30 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3831 58 3H-QNB -93 30 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3831 58 3H-QNB -93 30 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 2893 112 3H-QNB -27 66 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 3H-QNB -27 66 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 3H-QNB -27 66 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 3H-QNB -27 66 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398737 955 93 3H-NMS -10 92 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 955 93 3H-NMSP -10 92 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-NMS -10 92 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-NMSP -10 92 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-NMS -10 92 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-NMSP -10 92 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-NMS -10 92 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-NMSP -10 92 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-NMS -10 92 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-NMSP -10 92 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
9905731 168484 0 UNDEFINED -1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 334 6 1 5 2.2 CN(C)C1(CNCCC2CCOCC2)COc2ccccc2OC1 None
CHEMBL435353 168484 0 UNDEFINED -1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 334 6 1 5 2.2 CN(C)C1(CNCCC2CCOCC2)COc2ccccc2OC1 None
367 3795 12 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
5487427 3795 12 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
8592 3795 12 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL1900528 3795 12 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL3305968 3795 12 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL4650755 3795 12 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
DB01409 3795 12 None 2 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
154734599 2486 12 3H-NMS -19 12 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2486 12 3H-NMS -19 12 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2486 12 3H-NMS -19 12 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2486 12 3H-NMS -19 12 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
277 1289 62 3H-QNB -11 46 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1289 62 3H-QNB -11 46 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1289 62 3H-QNB -11 46 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1289 62 3H-QNB -11 46 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1289 62 3H-QNB -11 46 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
4919 206211 23 3H-QNB -2 9 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
CHEMBL86715 206211 23 3H-QNB -2 9 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
180 400 56 3H-QNB -23 40 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 400 56 3H-QNB -23 40 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 400 56 3H-QNB -23 40 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 400 56 3H-QNB -23 40 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 400 56 3H-QNB -23 40 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
4601 206724 35 3H-QNB -1 17 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 206724 35 3H-QNB -1 17 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 206724 35 3H-QNB -1 17 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
1613 2333 53 3H-QNB -19 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2333 53 3H-QNB -19 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2333 53 3H-QNB -19 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2333 53 3H-QNB -19 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2333 53 3H-QNB -19 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2200 3109 46 3H-4-DAMP -7 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 3H-4-DAMP -7 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 3H-4-DAMP -7 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 3H-4-DAMP -7 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 3H-4-DAMP -7 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
154825138 216012 0 3H-PIRENZEPINE -30 12 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
442108 84607 6 3H-QNB -1 12 Human 4.9 pKi = 4.9 Binding
NoneNone
PDSP KiDatabase 310 2 1 2 3.9 CC[C@H]1C[C@H]2C[C@H]3c4[nH]c5ccc(OC)cc5c4CCN(C2)[C@@H]13 None
CHEMBL222287 84607 6 3H-QNB -1 12 Human 4.9 pKi = 4.9 Binding
NoneNone
PDSP KiDatabase 310 2 1 2 3.9 CC[C@H]1C[C@H]2C[C@H]3c4[nH]c5ccc(OC)cc5c4CCN(C2)[C@@H]13 None
135398745 2893 112 35S-GTPGammaS -27 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 35S-GTPGammaS -27 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 35S-GTPGammaS -27 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 35S-GTPGammaS -27 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2745 3832 42 3H-NMS -21 9 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3832 42 3H-NMS -21 9 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3832 42 3H-NMS -21 9 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3832 42 3H-NMS -21 9 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3832 42 3H-NMS -21 9 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3832 42 3H-NMS -21 9 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
101 3793 24 3H-QNB -5248 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
55752 3793 24 3H-QNB -5248 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL35057 3793 24 3H-QNB -5248 14 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
2337 3232 77 3H-QNB -81 63 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3232 77 3H-QNB -81 63 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3232 77 3H-QNB -81 63 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3232 77 3H-QNB -81 63 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3232 77 3H-QNB -81 63 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135398745 2893 112 3H-NMS -27 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2893 112 3H-QNB -27 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 3H-NMS -27 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 3H-QNB -27 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 3H-NMS -27 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 3H-QNB -27 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 3H-NMS -27 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 3H-QNB -27 66 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3947 206372 53 3H-QNB -4 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
CHEMBL87708 206372 53 3H-QNB -4 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
2865 4112 73 3H-QNB -812 54 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4112 73 3H-QNB -812 54 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4112 73 3H-QNB -812 54 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4112 73 3H-QNB -812 54 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4112 73 3H-QNB -812 54 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
68617 205504 62 3H-QNB -12 26 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 205504 62 3H-QNB -12 26 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 205504 62 3H-QNB -12 26 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
154734599 2486 12 3H-NMS -66 12 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2486 12 3H-NMS -66 12 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2486 12 3H-NMS -66 12 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2486 12 3H-NMS -66 12 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
135398745 2893 112 3H-NMS -27 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2893 112 3H-NMSP -27 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 3H-NMS -27 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 3H-NMSP -27 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 3H-NMS -27 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 3H-NMSP -27 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 3H-NMS -27 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 3H-NMSP -27 66 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2337 3232 77 3H-QNB -81 63 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3232 77 3H-NMS -257 63 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3232 77 3H-QNB -81 63 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3232 77 3H-NMS -257 63 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3232 77 3H-QNB -81 63 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3232 77 3H-NMS -257 63 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3232 77 3H-QNB -81 63 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3232 77 3H-NMS -257 63 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3232 77 3H-QNB -81 63 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3232 77 3H-NMS -257 63 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2200 3109 46 3H-NMS -7 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 3H-NMS -7 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 3H-NMS -7 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 3H-NMS -7 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 3H-NMS -7 13 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
135398737 955 93 3H-NMS -7 92 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 955 93 3H-QNB -7 92 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-NMS -7 92 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-QNB -7 92 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-NMS -7 92 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-QNB -7 92 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-NMS -7 92 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-QNB -7 92 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-NMS -7 92 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-QNB -7 92 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
44431386 149001 0 UNDEFINED -1 3 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 332 5 1 5 2.1 CN(C)C1(CNCC=C2CCOCC2)COc2ccccc2OC1 None
CHEMBL394255 149001 0 UNDEFINED -1 3 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 332 5 1 5 2.1 CN(C)C1(CNCC=C2CCOCC2)COc2ccccc2OC1 None
154825138 216012 0 3H-NMS -17 12 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
154734599 2486 12 3H-NMS -66 12 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2486 12 3H-NMS -66 12 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2486 12 3H-NMS -66 12 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2486 12 3H-NMS -66 12 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
10090005 215961 0 3H-QNB -1778 11 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 361 1 0 3 4.4 CN1CCN(CC1)C2=CC3=C(C=CC(=C3)Cl)C(=CC#N)C4=CC=CC=C42 None
154825138 216012 0 3H-NMS -30 12 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
1212 1649 50 3H-QNB -407 66 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1649 50 3H-QNB -407 66 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1649 50 3H-QNB -407 66 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1649 50 3H-QNB -407 66 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1649 50 3H-QNB -407 66 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1212 1649 50 3H-QNB -2884 66 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1649 50 3H-QNB -2884 66 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1649 50 3H-QNB -2884 66 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1649 50 3H-QNB -2884 66 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1649 50 3H-QNB -2884 66 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
100 3776 58 3H-QNB -8 56 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3776 58 3H-QNB -8 56 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3776 58 3H-QNB -8 56 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3776 58 3H-QNB -8 56 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3776 58 3H-QNB -8 56 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
None 216231 0 3H-NMS 1 5 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 851 24 12 12 -2.6 CCC(C)C(C(=O)NC(CC(=O)O)C(=O)O)NC(=O)C(CO)NC(=O)C(CC1=CN=CN1)NC(=O)C(CC2=CN=CN2)NC(=O)C(CC3=CC=CC=C3)NC(=O)C4CCCN4 None
None 216231 0 3H-4-DAMP 1 5 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 851 24 12 12 -2.6 CCC(C)C(C(=O)NC(CC(=O)O)C(=O)O)NC(=O)C(CO)NC(=O)C(CC1=CN=CN1)NC(=O)C(CC2=CN=CN2)NC(=O)C(CC3=CC=CC=C3)NC(=O)C4CCCN4 None
2200 3109 46 3H-QNB -7 13 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 3H-QNB -7 13 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 3H-QNB -7 13 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 3H-QNB -7 13 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 3H-QNB -7 13 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
15387 45792 55 3H-QNB -2238 24 Rat 4.8 pKi = 4.8 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45792 55 3H-QNB -2238 24 Rat 4.8 pKi = 4.8 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
4839 216349 0 3H-NMS -4 5 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 323 5 0 3 3.8 CCN1CCCC(C1)OC(=O)C(C2=CC=CC=C2)C3=CC=CC=C3 None
15897 2840 0 3H-QNB -32 37 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2840 0 3H-QNB -32 37 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2840 0 3H-QNB -32 37 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
2200 3109 46 3H-PIRENZEPINE -11 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 3H-PIRENZEPINE -11 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 3H-PIRENZEPINE -11 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 3H-PIRENZEPINE -11 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 3H-PIRENZEPINE -11 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
None 216213 0 3H-QNB -38018 30 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
124226 1908 0 3H-NMS -1 5 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 315 6 1 2 4.7 OC(c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
322 1908 0 3H-NMS -1 5 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 315 6 1 2 4.7 OC(c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
71202 216346 0 3H-NMS -5 5 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 340 3 0 3 4.9 CC1(C2=CC=CC=C2N(C3=CC=CC=C31)C(=O)SCCN(C)C)C None
1353 1898 93 3H-NMS -2344 86 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1898 93 3H-QNB -2344 86 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1898 93 3H-NMS -2344 86 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1898 93 3H-QNB -2344 86 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1898 93 3H-NMS -2344 86 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1898 93 3H-QNB -2344 86 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1898 93 3H-NMS -2344 86 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1898 93 3H-QNB -2344 86 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1898 93 3H-NMS -2344 86 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1898 93 3H-QNB -2344 86 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
11954259 215954 0 3H-QNB -13182 44 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
154734599 2486 12 3H-NMS -66 12 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2486 12 3H-NMS -66 12 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2486 12 3H-NMS -66 12 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2486 12 3H-NMS -66 12 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
2200 3109 46 3H-NMS -11 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 3H-NMS -11 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 3H-NMS -11 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 3H-NMS -11 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 3H-NMS -11 13 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
44431369 87954 0 UNDEFINED 2 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 6 1 4 2.9 Cc1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 None
CHEMBL234253 87954 0 UNDEFINED 2 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 6 1 4 2.9 Cc1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 None
2200 3109 46 3H-NMS -7 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 3H-NMS -7 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 3H-NMS -7 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 3H-NMS -7 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 3H-NMS -7 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
132947 3835 9 3H-NMS -999 9 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
361 3835 9 3H-NMS -999 9 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
CHEMBL265256 3835 9 3H-NMS -999 9 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
209 3035 97 3H-QNB -144 23 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3035 97 3H-QNB -144 23 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3035 97 3H-QNB -144 23 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3035 97 3H-QNB -144 23 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3035 97 3H-QNB -144 23 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1615 167767 24 3H-QNB -5 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167767 24 3H-QNB -5 45 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
209 3035 97 3H-QNB -2630 23 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3035 97 3H-QNB -2630 23 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3035 97 3H-QNB -2630 23 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3035 97 3H-QNB -2630 23 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3035 97 3H-QNB -2630 23 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
44431376 87288 0 UNDEFINED 2 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 344 6 1 4 2.7 CN(C)C1(CNCCc2ccccc2F)COc2ccccc2OC1 None
CHEMBL233200 87288 0 UNDEFINED 2 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 344 6 1 4 2.7 CN(C)C1(CNCCc2ccccc2F)COc2ccccc2OC1 None
2337 3232 77 3H-QNB -81 63 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3232 77 3H-QNB -81 63 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3232 77 3H-QNB -81 63 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3232 77 3H-QNB -81 63 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3232 77 3H-QNB -81 63 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
16362 3103 71 3H-QNB -10232 30 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3103 71 3H-QNB -10232 30 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3103 71 3H-QNB -10232 30 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3103 71 3H-QNB -10232 30 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3103 71 3H-QNB -10232 30 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
16362 3103 71 3H-QNB -562 30 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3103 71 3H-QNB -562 30 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3103 71 3H-QNB -562 30 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3103 71 3H-QNB -562 30 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3103 71 3H-QNB -562 30 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
154734599 2486 12 3H-4-DAMP -19 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2486 12 3H-4-DAMP -19 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2486 12 3H-4-DAMP -19 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2486 12 3H-4-DAMP -19 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
12057539 208018 42 3H-NMS -2 21 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 3H-NMS -2 21 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 3H-NMS -2 21 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
None 216202 0 3H-NMS -1 6 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 426 7 1 3 4.0 C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5 None
16721019 87957 0 UNDEFINED -1 3 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 7 2 5 2.5 CN(C)C1(CNCCC2CCC(CO)CC2)COc2ccccc2OC1 None
CHEMBL234258 87957 0 UNDEFINED -1 3 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 362 7 2 5 2.5 CN(C)C1(CNCCC2CCC(CO)CC2)COc2ccccc2OC1 None
12057539 208018 42 3H-NMS -2 21 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 3H-NMS -2 21 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 3H-NMS -2 21 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
None 216230 0 3H-NMS -1 5 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 311 3 1 2 3.9 C1CCC(CC1)C(C#CCN2CCCCC2)(C3=CC=CC=C3)O None
1734 116 10 3H-NMS -2 13 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 10 3H-NMS -2 13 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 10 3H-NMS -2 13 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
2745 3832 42 3H-NMS -21 9 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3832 42 3H-NMS -21 9 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3832 42 3H-NMS -21 9 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3832 42 3H-NMS -21 9 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3832 42 3H-NMS -21 9 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3832 42 3H-NMS -21 9 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
44431382 87992 0 UNDEFINED 2 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 332 6 1 4 3.3 CN(C)C1(CNCCC2CCCCC2)COc2ccccc2OC1 None
CHEMBL234438 87992 0 UNDEFINED 2 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 332 6 1 4 3.3 CN(C)C1(CNCCC2CCCCC2)COc2ccccc2OC1 None
2905 14466 50 3H-NMS -1 5 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 None
CHEMBL1201338 14466 50 3H-NMS -1 5 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 None
44431383 87993 0 UNDEFINED -1 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 346 6 1 4 3.7 CN(C)C1(CNCCC2CCCCCC2)COc2ccccc2OC1 None
CHEMBL234439 87993 0 UNDEFINED -1 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 346 6 1 4 3.7 CN(C)C1(CNCCC2CCCCCC2)COc2ccccc2OC1 None
1734 116 10 3H-NMS -2 13 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 10 3H-NMS -2 13 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 10 3H-NMS -2 13 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
44431389 146126 0 UNDEFINED -1 3 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 348 6 2 5 2.3 CN(C)C1(CNCCC2CCC(O)CC2)COc2ccccc2OC1 None
CHEMBL391977 146126 0 UNDEFINED -1 3 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 348 6 2 5 2.3 CN(C)C1(CNCCC2CCC(O)CC2)COc2ccccc2OC1 None
2745 3832 42 3H-NMS -3 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3832 42 3H-NMS -3 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3832 42 3H-NMS -3 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3832 42 3H-NMS -3 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3832 42 3H-NMS -3 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3832 42 3H-NMS -3 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
135398737 955 93 3H-QNB -10 92 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-QNB -10 92 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-QNB -10 92 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-QNB -10 92 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-QNB -10 92 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
44431367 87953 0 UNDEFINED 4 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 6 1 4 2.6 CN(C)C1(CNCCc2ccccc2)COc2ccccc2OC1 None
CHEMBL234252 87953 0 UNDEFINED 4 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 6 1 4 2.6 CN(C)C1(CNCCc2ccccc2)COc2ccccc2OC1 None
44431370 87955 0 UNDEFINED 2 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 360 6 1 4 3.2 CN(C)C1(CNCCc2ccc(Cl)cc2)COc2ccccc2OC1 None
CHEMBL234254 87955 0 UNDEFINED 2 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 360 6 1 4 3.2 CN(C)C1(CNCCc2ccc(Cl)cc2)COc2ccccc2OC1 None
5831 215938 0 3H-QNB -51 12 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
11976 917 59 3H-QNB -20 24 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 917 59 3H-QNB -20 24 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 917 59 3H-QNB -20 24 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 917 59 3H-QNB -20 24 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
2995 204382 53 3H-QNB -5 23 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204382 53 3H-QNB -5 23 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204382 53 3H-QNB -5 23 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
154734599 2486 12 3H-NMS -19 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2486 12 3H-NMS -19 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2486 12 3H-NMS -19 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2486 12 3H-NMS -19 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
11976 917 59 3H-QNB -12 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 917 59 3H-QNB -12 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 917 59 3H-QNB -12 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 917 59 3H-QNB -12 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
1979 77297 70 3H-cAMP 2 4 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
CHEMBL20835 77297 70 3H-cAMP 2 4 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 None
2200 3109 46 3H-NMS -7 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 3H-NMS -7 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 3H-NMS -7 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 3H-NMS -7 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 3H-NMS -7 13 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
132947 3835 9 3H-NMS -999 9 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
361 3835 9 3H-NMS -999 9 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
CHEMBL265256 3835 9 3H-NMS -999 9 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
3012003 216119 0 3H-QNB -1 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 311 5 0 3 3.8 CN1CCC(C(C1)COC2=CC=C(C=C2)OC)C3=CC=CC=C3 None
2200 3109 46 3H-NMS -11 13 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 3H-NMS -11 13 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 3H-NMS -11 13 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 3H-NMS -11 13 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 3H-NMS -11 13 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
1224 1420 83 3H-QNB -5 13 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1420 83 3H-QNB -5 13 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1420 83 3H-QNB -5 13 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1420 83 3H-QNB -5 13 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1420 83 3H-QNB -5 13 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1420 83 3H-QNB -5 13 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
44431375 87287 0 UNDEFINED 2 3 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 394 6 1 4 3.9 CN(C)C1(CNCCc2c(Cl)cccc2Cl)COc2ccccc2OC1 None
CHEMBL233199 87287 0 UNDEFINED 2 3 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 394 6 1 4 3.9 CN(C)C1(CNCCc2c(Cl)cccc2Cl)COc2ccccc2OC1 None
None 216109 0 3H-QNB -2511 24 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
100 3776 58 3H-QNB -12 56 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3776 58 3H-QNB -12 56 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3776 58 3H-QNB -12 56 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3776 58 3H-QNB -12 56 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3776 58 3H-QNB -12 56 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
187 255 39 3H-NMS -34 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
294 255 39 3H-NMS -34 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
65 255 39 3H-NMS -34 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
8593 255 39 3H-NMS -34 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
CHEMBL667 255 39 3H-NMS -34 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
DB03128 255 39 3H-NMS -34 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
135398737 955 93 3H-QNB -10 92 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-QNB -10 92 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-QNB -10 92 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-QNB -10 92 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-QNB -10 92 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398745 2893 112 3H-NMS -16 66 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2893 112 3H-QNB -16 66 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 3H-NMS -16 66 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 3H-QNB -16 66 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 3H-NMS -16 66 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 3H-QNB -16 66 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 3H-NMS -16 66 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 3H-QNB -16 66 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398737 955 93 3H-QNB -7 92 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-QNB -7 92 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-QNB -7 92 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-QNB -7 92 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-QNB -7 92 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1613 2333 53 3H-QNB -70 45 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2333 53 3H-QNB -70 45 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2333 53 3H-QNB -70 45 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2333 53 3H-QNB -70 45 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2333 53 3H-QNB -70 45 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2435 3563 83 3H-QNB -5248 49 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3563 83 3H-QNB -5248 49 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3563 83 3H-QNB -5248 49 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3563 83 3H-QNB -5248 49 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3563 83 3H-QNB -5248 49 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2435 3563 83 3H-QNB -239 49 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3563 83 3H-QNB -239 49 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3563 83 3H-QNB -239 49 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3563 83 3H-QNB -239 49 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3563 83 3H-QNB -239 49 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
154734599 2486 12 3H-NMS -19 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2486 12 3H-NMS -19 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2486 12 3H-NMS -19 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2486 12 3H-NMS -19 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
108107 79915 38 3H-NMS -4 16 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
156592250 79915 38 3H-NMS -4 16 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL1256878 79915 38 3H-NMS -4 16 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL212579 79915 38 3H-NMS -4 16 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
None 217050 0 UNDEFINED - 1 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 284 4 1 2 4.8 CC1=C(C=C(C=C1NC2CC2)C3CC3)N4CCCCCC4 None
44431381 148997 0 UNDEFINED -1 3 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 318 6 1 4 2.9 CN(C)C1(CNCCC2CCCC2)COc2ccccc2OC1 None
CHEMBL394254 148997 0 UNDEFINED -1 3 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 318 6 1 4 2.9 CN(C)C1(CNCCC2CCCC2)COc2ccccc2OC1 None
71128 96781 25 3H-NMS -3 8 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 None
CHEMBL26505 96781 25 3H-NMS -3 8 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 325 8 0 3 3.9 CCN(CC)CCOC(=O)C(C)(c1ccccc1)c1ccccc1 None
1734 116 10 3H-NMS -2 13 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
307 116 10 3H-NMS -2 13 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
CHEMBL168067 116 10 3H-NMS -2 13 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C None
2381 660 48 3H-QNB -9 9 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
374 660 48 3H-QNB -9 9 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
7128 660 48 3H-QNB -9 9 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
CHEMBL1101 660 48 3H-QNB -9 9 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
DB00810 660 48 3H-QNB -9 9 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 None
310 1909 0 3H-NMS 3 11 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
3602 1909 0 3H-NMS 3 11 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
CHEMBL3545990 1909 0 3H-NMS 3 11 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 None
154734599 2486 12 3H-NMS -66 12 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2486 12 3H-NMS -66 12 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2486 12 3H-NMS -66 12 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2486 12 3H-NMS -66 12 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
154734599 2486 12 3H-PIRENZEPINE -66 12 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 2486 12 3H-PIRENZEPINE -66 12 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 2486 12 3H-PIRENZEPINE -66 12 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 2486 12 3H-PIRENZEPINE -66 12 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
62865 1263 0 3H-4-DAMP -5 15 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
746 1263 0 3H-4-DAMP -5 15 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
84 1263 0 3H-4-DAMP -5 15 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
CHEMBL2104153 1263 0 3H-4-DAMP -5 15 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
DB09000 1263 0 3H-4-DAMP -5 15 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
2200 3109 46 3H-NMS -11 13 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 3H-NMS -11 13 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 3H-NMS -11 13 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 3H-NMS -11 13 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 3H-NMS -11 13 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
46780481 107504 20 3H-NMS -776 54 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107504 20 3H-NMS -776 54 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107504 20 3H-NMS -776 54 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107504 20 3H-NMS -776 54 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
3337 206344 27 3H-QNB -158 41 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-QNB -158 41 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-QNB -158 41 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-QNB -158 41 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-QNB -158 41 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
114743 216075 0 3H-QNB -2 8 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 291 1 1 1 4.9 C1CC(C2=CC=CC=C2C1C3=CC(=C(C=C3)Cl)Cl)N None
None 216228 0 3H-NMS -3090 21 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
20980871 216403 0 3H-QNB -9 8 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 3 0 2 4.7 CN(C)CCC=C1C2=CC=CC=C2CSC3=CC=CC=C31 None
2774 3839 95 3H-NMS -2 10 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593 3839 95 3H-NMS -2 10 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
7319 3839 95 3H-NMS -2 10 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
CHEMBL1200604 3839 95 3H-NMS -2 10 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB00809 3839 95 3H-NMS -2 10 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB01199 3839 95 3H-NMS -2 10 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
132947 3835 9 3H-NMS -309 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
361 3835 9 3H-NMS -309 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
CHEMBL265256 3835 9 3H-NMS -309 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C None
180 400 56 3H-Arachidonic Acid -23 40 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 400 56 3H-Arachidonic Acid -23 40 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 400 56 3H-Arachidonic Acid -23 40 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 400 56 3H-Arachidonic Acid -23 40 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 400 56 3H-Arachidonic Acid -23 40 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
3652 4066 79 3H-QNB -3 18 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4066 79 3H-QNB -3 18 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4066 79 3H-QNB -3 18 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4066 79 3H-QNB -3 18 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4066 79 3H-QNB -3 18 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
1613 2333 53 3H-QNB -19 45 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2333 53 3H-QNB -19 45 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2333 53 3H-QNB -19 45 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2333 53 3H-QNB -19 45 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2333 53 3H-QNB -19 45 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2337 3232 77 3H-QNB -257 63 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3232 77 3H-QNB -257 63 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3232 77 3H-QNB -257 63 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3232 77 3H-QNB -257 63 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3232 77 3H-QNB -257 63 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
10938 1689 0 None -1 4 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
299 1689 0 None -1 4 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
3256 1689 0 None -1 4 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
CHEMBL2110739 1689 0 None -1 4 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C None
2370 620 31 None 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
297 620 31 None 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
358 620 31 None 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
CHEMBL1482 620 31 None 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
DB01019 620 31 None 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N None
44431391 146396 0 UNDEFINED 1 3 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 352 6 1 5 2.3 CN(C)C1(CNCCC2CCOCC2)COc2ccc(F)cc2OC1 None
CHEMBL392186 146396 0 UNDEFINED 1 3 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 352 6 1 5 2.3 CN(C)C1(CNCCC2CCOCC2)COc2ccc(F)cc2OC1 None
187 255 39 3H-NMS -26 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
294 255 39 3H-NMS -26 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
65 255 39 3H-NMS -26 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
8593 255 39 3H-NMS -26 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
CHEMBL667 255 39 3H-NMS -26 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
DB03128 255 39 3H-NMS -26 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
44431380 87956 0 UNDEFINED 2 3 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 318 5 1 4 2.9 CN(C)C1(CNCC2CCCCC2)COc2ccccc2OC1 None
CHEMBL234257 87956 0 UNDEFINED 2 3 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 318 5 1 4 2.9 CN(C)C1(CNCC2CCCCC2)COc2ccccc2OC1 None
279 1648 26 3H-QNB -8 18 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 1648 26 3H-QNB -8 18 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 1648 26 3H-QNB -8 18 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
187 255 39 3H-NMS -26 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
294 255 39 3H-NMS -26 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
65 255 39 3H-NMS -26 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
8593 255 39 3H-NMS -26 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
CHEMBL667 255 39 3H-NMS -26 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
DB03128 255 39 3H-NMS -26 9 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C None
2230 464 60 3H-QNB -588 10 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C None
296 464 60 3H-QNB -588 10 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C None
CHEMBL7303 464 60 3H-QNB -588 10 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C None
DB04365 464 60 3H-QNB -588 10 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C None
100 3776 58 3H-QNB -8 56 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3776 58 3H-QNB -8 56 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3776 58 3H-QNB -8 56 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3776 58 3H-QNB -8 56 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3776 58 3H-QNB -8 56 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
135398745 2893 112 3H-QNB -16 66 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 3H-QNB -16 66 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 3H-QNB -16 66 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 3H-QNB -16 66 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
7534 216347 0 3H-NMS -4 5 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 291 3 1 4 2.5 CC1CC(CC(N1C)(C)C)OC(=O)C(C2=CC=CC=C2)O None
None 216230 0 3H-NMS -1 5 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 311 3 1 2 3.9 C1CCC(CC1)C(C#CCN2CCCCC2)(C3=CC=CC=C3)O None
2200 3109 46 3H-NMS -11 13 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 3H-NMS -11 13 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 3H-NMS -11 13 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 3H-NMS -11 13 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 3H-NMS -11 13 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
134 2497 24 3H-QNB -134 68 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 3H-QNB -134 68 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 3H-QNB -134 68 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 3H-QNB -134 68 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 3H-QNB -134 68 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
242 469 124 3H-QNB -114 52 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 469 124 3H-QNB -114 52 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 469 124 3H-QNB -114 52 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 469 124 3H-QNB -114 52 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 469 124 3H-QNB -114 52 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 469 124 3H-QNB -3388 52 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 469 124 3H-QNB -3388 52 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 469 124 3H-QNB -3388 52 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 469 124 3H-QNB -3388 52 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 469 124 3H-QNB -3388 52 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 469 124 3H-QNB -114 52 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 469 124 3H-QNB -114 52 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 469 124 3H-QNB -114 52 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 469 124 3H-QNB -114 52 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 469 124 3H-QNB -114 52 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2726 916 68 3H-QNB -18 73 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 916 68 3H-QNB -18 73 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 916 68 3H-QNB -18 73 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 916 68 3H-QNB -18 73 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 916 68 3H-QNB -18 73 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1192 147 47 3H-NMS -75 17 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
1794 147 47 3H-NMS -75 17 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
CHEMBL501701 147 47 3H-NMS -75 17 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
1353 1898 93 None -154 86 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1898 93 None -154 86 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1898 93 None -154 86 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1898 93 None -154 86 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1898 93 None -154 86 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1830 2572 44 None -39 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2572 44 None -39 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2572 44 None -39 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2572 44 None -39 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2572 44 None -39 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
2389 3306 118 None -602 68 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3306 118 None -602 68 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3306 118 None -602 68 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3306 118 None -602 68 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3306 118 None -602 68 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2865 4112 73 None -812 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4112 73 None -812 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4112 73 None -812 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4112 73 None -812 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4112 73 None -812 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2448 99295 70 None -134 18 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
CHEMBL28218 99295 70 None -134 18 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
42470 216157 0 3H-NMS -14 6 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 345 10 0 3 4.9 CCN(CCCC(=O)C1CCCCC1)C(C)CC2=CC=C(C=C2)OC None
4066 204603 78 3H-QNB 1 7 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
CHEMBL73451 204603 78 3H-QNB 1 7 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
3652 46214 70 None -1 9 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
CHEMBL1535 46214 70 None -1 9 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 335 9 2 4 3.8 CCN(CCO)CCCC(C)Nc1ccnc2cc(Cl)ccc12 None
242 469 124 None -114 52 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 469 124 None -114 52 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 469 124 None -114 52 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 469 124 None -114 52 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 469 124 None -114 52 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
66265 93984 15 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL248702 93984 15 None -1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
212 3777 47 None -5 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3777 47 None -5 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3777 47 None -5 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3777 47 None -5 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3777 47 None -5 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
448537 160226 89 None -28 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
CHEMBL411 160226 89 None -28 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
28417 40009 49 None -1 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C None
CHEMBL1479 40009 49 None -1 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C None
2719 914 74 None -3 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
5535 914 74 None -3 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
607 914 74 None -3 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
CHEMBL76 914 74 None -3 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
DB00608 914 74 None -3 11 Human 8.3 pKi = 8.3 Binding
Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNBActivity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug Central 319 8 1 3 4.8 CCN(CCCC(Nc1ccnc2c1ccc(c2)Cl)C)CC None
441383 20301 57 None -6 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL1306 20301 57 None -6 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
2435 3563 83 None -239 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3563 83 None -239 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3563 83 None -239 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3563 83 None -239 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3563 83 None -239 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2812 4747 101 None -22 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4747 101 None -22 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
16362 3103 71 None -562 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3103 71 None -562 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3103 71 None -562 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3103 71 None -562 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3103 71 None -562 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
209 3035 97 None -144 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3035 97 None -144 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3035 97 None -144 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3035 97 None -144 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3035 97 None -144 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2337 3232 77 None -81 63 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3232 77 None -81 63 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3232 77 None -81 63 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3232 77 None -81 63 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3232 77 None -81 63 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
44431388 87290 0 UNDEFINED 2 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 348 6 1 5 2.8 CN(C)C1(CNCCC2=CCSCC2)COc2ccccc2OC1 None
CHEMBL233202 87290 0 UNDEFINED 2 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 348 6 1 5 2.8 CN(C)C1(CNCCC2=CCSCC2)COc2ccccc2OC1 None
3389 217683 0 None -1 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
1836 2574 59 None -42 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
3340 2574 59 None -42 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
5281040 2574 59 None -42 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
CHEMBL787 2574 59 None -42 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
DB00471 2574 59 None -42 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
107782 14436 18 None -1 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O None
67151996 14436 18 None -1 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O None
CHEMBL1201207 14436 18 None -1 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O None
68617 205504 62 None -12 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 205504 62 None -12 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 205504 62 None -12 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
308 2047 23 3H-NMS 1 9 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
3603 2047 23 3H-NMS 1 9 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
CHEMBL1256682 2047 23 3H-NMS 1 9 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O None
1971 2846 38 3H-QNB -4 30 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2846 38 3H-QNB -4 30 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2846 38 3H-QNB -4 30 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2846 38 3H-QNB -4 30 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2846 38 3H-QNB -4 30 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
15897 2840 0 3H-QNB -32 37 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2840 0 3H-QNB -32 37 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2840 0 3H-QNB -32 37 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
135398745 2893 112 3H-QNB -27 66 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 3H-QNB -27 66 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 3H-QNB -27 66 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 3H-QNB -27 66 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
5831 215938 0 3H-NMS -51 12 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 182 3 1 2 -3.2 C[N+](C)(C)CCOC(=O)N.[Cl-] None
1225 1459 26 3H-QNB -69 22 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1459 26 3H-QNB -69 22 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1459 26 3H-QNB -69 22 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1459 26 3H-QNB -69 22 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1459 26 3H-QNB -69 22 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
6450478 215987 0 3H-QNB -13 12 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 340 0 0 6 3.4 CN1CCN(CC1)C2=NC3=CSC=C3C(=CC#N)C4=CSC=C42 None
44431372 87286 0 UNDEFINED -1 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 368 7 1 4 3.7 CC(C)c1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 None
CHEMBL233198 87286 0 UNDEFINED -1 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 368 7 1 4 3.7 CC(C)c1ccc(CCNCC2(N(C)C)COc3ccccc3OC2)cc1 None
2865 4112 73 3H-QNB -11481 54 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4112 73 3H-QNB -11481 54 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4112 73 3H-QNB -11481 54 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4112 73 3H-QNB -11481 54 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4112 73 3H-QNB -11481 54 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
73707487 216348 0 3H-NMS -8 9 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 355 3 1 4 2.5 CN1C2CCC1CC(C2)OC(=O)C(C3=CC=CC=C3)O.Br None
1212 1649 50 None -407 66 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1649 50 None -407 66 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1649 50 None -407 66 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1649 50 None -407 66 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1649 50 None -407 66 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1209 1645 75 None -30 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1645 75 None -30 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1645 75 None -30 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1645 75 None -30 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1645 75 None -30 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
214 3831 58 None -93 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3831 58 None -93 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3831 58 None -93 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3831 58 None -93 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3831 58 None -93 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3831 58 None -93 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
657255 199061 34 None -11 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
CHEMBL588119 199061 34 None -11 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1 None
5353853 17954 47 None -13 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
9556529 17954 47 None -13 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1262 17954 47 None -13 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
11057 176125 23 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
3468 176125 23 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
CHEMBL459265 176125 23 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
CHEMBL64894 176125 23 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
5318 15544 49 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1200348 15544 49 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1221 15544 49 None -1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
176 397 66 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 397 66 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 397 66 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 397 66 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 397 66 None -1 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
4189 206899 96 None -12 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 206899 96 None -12 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 206899 96 None -12 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
4746 204868 31 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 None
CHEMBL1334033 204868 31 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 None
CHEMBL75880 204868 31 None -1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 None
1016 3720 78 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3720 78 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3720 78 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3720 78 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3720 78 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3720 78 None -12 35 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
1210 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1213 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2725 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
33036 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4411 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
616 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6976 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
716121 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
90475904 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 915 51 None -79 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6918558 14482 41 None -1 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 None
CHEMBL1201764 14482 41 None -1 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 None
1548955 88552 20 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2800 88552 20 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
CHEMBL2355051 88552 20 None -1 18 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2745 3832 42 3H-QNB -21 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
5572 3832 42 3H-QNB -21 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
66007 3832 42 3H-QNB -21 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
7315 3832 42 3H-QNB -21 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
CHEMBL1490 3832 42 3H-QNB -21 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
DB00376 3832 42 3H-QNB -21 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 None
191 402 98 None -37 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 402 98 None -37 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 402 98 None -37 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 402 98 None -37 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 402 98 None -37 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
3198 205490 76 None -10 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 205490 76 None -10 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 205490 76 None -10 34 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
2274 3151 58 None -21 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3151 58 None -21 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3151 58 None -21 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3151 58 None -21 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3151 58 None -21 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
12488 1644 56 None -8 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
941361 1644 56 None -8 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
CHEMBL30008 1644 56 None -8 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
DB04841 1644 56 None -8 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
135 2515 43 None -22 58 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2515 43 None -22 58 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2515 43 None -22 58 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2515 43 None -22 58 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2515 43 None -22 58 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
237 204842 48 None 1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL546257 204842 48 None 1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL554190 204842 48 None 1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
CHEMBL7568 204842 48 None 1 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12 None
1530 2169 50 None -57 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 2169 50 None -57 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 2169 50 None -57 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 2169 50 None -57 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 2169 50 None -57 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
2200 3109 46 None -7 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 None -7 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 None -7 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 None -7 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 None -7 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
1224 1420 83 None -5 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1420 83 None -5 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1420 83 None -5 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1420 83 None -5 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1420 83 None -5 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1420 83 None -5 13 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
2995 204382 53 None -5 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204382 53 None -5 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204382 53 None -5 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
21855 84217 42 None -14 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 None
CHEMBL22108 84217 42 None -14 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 None
72064 78372 14 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
Drug Central 318 8 0 4 3.1 CCN(CC)CCOC(=O)C(c1ccccc1)N1CCCCC1 None
CHEMBL2110892 78372 14 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysisDisplacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
Drug Central 318 8 0 4 3.1 CCN(CC)CCOC(=O)C(c1ccccc1)N1CCCCC1 None
2247 504 81 None -19 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 504 81 None -19 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 504 81 None -19 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 504 81 None -19 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 504 81 None -19 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
1547484 937 74 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
654 937 74 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
9072 937 74 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL43064 937 74 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB00568 937 74 None -5 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
6726 1269 51 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
7151 1269 51 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
749 1269 51 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL648 1269 51 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB01176 1269 51 None -6 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
44431387 87289 0 UNDEFINED 1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 350 6 1 5 2.9 CN(C)C1(CNCCC2CCSCC2)COc2ccccc2OC1 None
CHEMBL233201 87289 0 UNDEFINED 1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 350 6 1 5 2.9 CN(C)C1(CNCCC2CCSCC2)COc2ccccc2OC1 None
3191 102831 97 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102831 97 None -6 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
3947 206372 53 None -4 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
CHEMBL87708 206372 53 None -4 16 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 None
1613 2333 53 None -19 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2333 53 None -19 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2333 53 None -19 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2333 53 None -19 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2333 53 None -19 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1427 2000 54 3H-QNB -2 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2000 54 3H-QNB -2 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2000 54 3H-QNB -2 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2000 54 3H-QNB -2 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2000 54 3H-QNB -2 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
2726 916 68 3H-QNB -35 73 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 916 68 3H-QNB -35 73 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 916 68 3H-QNB -35 73 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 916 68 3H-QNB -35 73 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 916 68 3H-QNB -35 73 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
129989 450 51 3H-NMS -16 9 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC None
8584 450 51 3H-NMS -16 9 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC None
CHEMBL43383 450 51 3H-NMS -16 9 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC None
None 216232 0 3H-NMS -10 5 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 574 9 3 7 4.0 CCCN(CCC)CC1CCCCN1CCNC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4.CS(=O)(=O)O None
2726 916 68 3H-QNB -18 73 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 916 68 3H-QNB -18 73 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 916 68 3H-QNB -18 73 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 916 68 3H-QNB -18 73 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 916 68 3H-QNB -18 73 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
3337 206344 27 3H-QNB -158 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 3H-QNB -158 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 3H-QNB -158 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 3H-QNB -158 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 3H-QNB -158 41 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
4011 82379 49 None -14 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 82379 49 None -14 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
4976 203556 29 None -1 12 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
CHEMBL668 203556 29 None -1 12 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
135398737 955 93 3H-NMS -10 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 955 93 3H-QNB -10 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-NMS -10 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 3H-QNB -10 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-NMS -10 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 3H-QNB -10 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-NMS -10 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 3H-QNB -10 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-NMS -10 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 3H-QNB -10 92 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1712 2475 43 None -6 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2475 43 None -6 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2475 43 None -6 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2475 43 None -6 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2475 43 None -6 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
2284 3160 33 None -10 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3160 33 None -10 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3160 33 None -10 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3160 33 None -10 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3160 33 None -10 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
2335 11816 22 None -1 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
8478 11816 22 None -1 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
CHEMBL1182210 11816 22 None -1 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
CHEMBL221753 11816 22 None -1 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
135398745 2893 112 None -27 66 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2893 112 None -27 66 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2893 112 None -27 66 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2893 112 None -27 66 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
103 4122 61 None -144 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4122 61 None -144 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4122 61 None -144 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4122 61 None -144 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4122 61 None -144 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
1427 2000 54 None -2 27 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2000 54 None -2 27 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2000 54 None -2 27 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2000 54 None -2 27 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2000 54 None -2 27 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
4919 206211 23 3H-NMS -1 9 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
CHEMBL86715 206211 23 3H-NMS -1 9 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
2726 916 68 None -18 73 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 916 68 None -18 73 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 916 68 None -18 73 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 916 68 None -18 73 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 916 68 None -18 73 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
3055 1421 44 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
313 1421 44 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
7163 1421 44 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
CHEMBL936 1421 44 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
DB01231 1421 44 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 None
1225 1459 26 None -69 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1459 26 None -69 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1459 26 None -69 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1459 26 None -69 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1459 26 None -69 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
1971 2846 38 None -4 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2846 38 None -4 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2846 38 None -4 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2846 38 None -4 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2846 38 None -4 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
6075 150084 42 None -3 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
CHEMBL395110 150084 42 None -3 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
43815 186896 64 None -5 25 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186896 64 None -5 25 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186896 64 None -5 25 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
5284550 41691 15 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
CHEMBL1492500 41691 15 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 None
4601 206724 35 None -1 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 206724 35 None -1 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 206724 35 None -1 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
2398 951 62 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 951 62 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 951 62 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 951 62 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 951 62 None -1 29 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
124087 1377 114 None -9 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
7157 1377 114 None -9 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
814 1377 114 None -9 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
CHEMBL1172 1377 114 None -9 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
DB00967 1377 114 None -9 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
62865 1263 0 None -5 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
746 1263 0 None -5 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
84 1263 0 None -5 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
CHEMBL2104153 1263 0 None -5 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
DB09000 1263 0 None -5 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
2774 3839 95 None -2 10 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
5593 3839 95 None -2 10 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
7319 3839 95 None -2 10 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
CHEMBL1200604 3839 95 None -2 10 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB00809 3839 95 None -2 10 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
DB01199 3839 95 None -2 10 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 None
2200 3109 46 None -11 13 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 None -11 13 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 None -11 13 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 None -11 13 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 None -11 13 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
135398737 955 93 None -10 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 955 93 None -10 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 955 93 None -10 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 955 93 None -10 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 955 93 None -10 92 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
100 3776 58 None -8 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3776 58 None -8 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3776 58 None -8 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3776 58 None -8 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3776 58 None -8 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5387 94850 31 3H-NMS -4 6 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O None
CHEMBL253978 94850 31 3H-NMS -4 6 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 370 2 1 5 2.5 Cc1scc2c1N(C(=O)CN1CCN(C)CC1)c1ccccc1NC2=O None
73707487 216348 0 None -1 9 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 355 3 1 4 2.5 CN1C2CCC1CC(C2)OC(=O)C(C3=CC=CC=C3)O.Br None
3652 4066 79 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4066 79 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4066 79 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4066 79 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4066 79 None -3 18 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
180 400 56 None -23 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 400 56 None -23 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 400 56 None -23 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 400 56 None -23 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 400 56 None -23 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
4919 206211 23 None -2 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
CHEMBL86715 206211 23 None -2 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 None
2337 3232 77 3H-NMS -81 63 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3232 77 3H-NMS -81 63 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3232 77 3H-NMS -81 63 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3232 77 3H-NMS -81 63 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3232 77 3H-NMS -81 63 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1353 1898 93 3H-QNB -2344 86 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1898 93 3H-QNB -2344 86 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1898 93 3H-QNB -2344 86 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1898 93 3H-QNB -2344 86 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1898 93 3H-QNB -2344 86 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2448 99295 70 3H-QNB -5011 18 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
CHEMBL28218 99295 70 3H-QNB -5011 18 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
2448 99295 70 3H-QNB -134 18 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
CHEMBL28218 99295 70 3H-QNB -134 18 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
103 4122 61 3H-QNB -60 54 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4122 61 3H-QNB -60 54 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4122 61 3H-QNB -60 54 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4122 61 3H-QNB -60 54 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4122 61 3H-QNB -60 54 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2200 3109 46 3H-NMS -11 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 3H-NMS -11 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 3H-NMS -11 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 3H-NMS -11 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 3H-NMS -11 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
103 4122 61 3H-QNB -144 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4122 61 3H-QNB -144 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4122 61 3H-QNB -144 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4122 61 3H-QNB -144 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4122 61 3H-QNB -144 54 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
208 2843 0 3H-QNB -8 13 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
4541 2843 0 3H-QNB -8 13 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL1494 2843 0 3H-QNB -8 13 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 4.2 NCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
154059 3610 51 None 1 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
2457 3610 51 None 1 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
7483 3610 51 None 1 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
CHEMBL1734 3610 51 None 1 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
DB01591 3610 51 None 1 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamineBinding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
Drug Central 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 None
277 1289 62 None -11 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1289 62 None -11 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1289 62 None -11 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1289 62 None -11 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1289 62 None -11 46 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
26987 946 33 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 946 33 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 946 33 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 946 33 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 946 33 None -56 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
2705 3813 64 None -1 10 Rat 8.1 pKi = 8.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
360 3813 64 None -1 10 Rat 8.1 pKi = 8.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
443879 3813 64 None -1 10 Rat 8.1 pKi = 8.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
CHEMBL1382 3813 64 None -1 10 Rat 8.1 pKi = 8.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
DB01036 3813 64 None -1 10 Rat 8.1 pKi = 8.1 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
4904 155497 48 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 5 1 2 3.8 OC(CCN1CCCCC1)(c1ccccc1)c1ccccc1 None
CHEMBL404215 155497 48 None -1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 295 5 1 2 3.8 OC(CCN1CCCCC1)(c1ccccc1)c1ccccc1 None
5648 78382 9 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 None
CHEMBL2107687 78382 9 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 None
CHEMBL2111176 78382 9 None -1 5 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1 None
2286 3161 51 None -1 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3161 51 None -1 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3161 51 None -1 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3161 51 None -1 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3161 51 None -1 30 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
2705 3813 64 None -1 10 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
360 3813 64 None -1 10 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
443879 3813 64 None -1 10 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
CHEMBL1382 3813 64 None -1 10 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
DB01036 3813 64 None -1 10 Human 8.1 pKi = 8.1 Binding
Binding affinity to human muscarinic M3 receptorBinding affinity to human muscarinic M3 receptor
Drug Central 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O None
10470 2471 7 None -11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
Drug Central 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C None
1689 2471 7 None -11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
Drug Central 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C None
4057 2471 7 None -11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
Drug Central 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C None
CHEMBL524004 2471 7 None -11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
Drug Central 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C None
DB04843 2471 7 None -11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]NMS from human M3R expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
Drug Central 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C None
319 1312 44 None -3 9 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
321 1312 44 None -3 9 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
444031 1312 44 None -3 9 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
784 1312 44 None -3 9 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
CHEMBL1346 1312 44 None -3 9 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
DB00496 1312 44 None -3 9 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular glandDisplacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
1371 1910 11 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
24199 1910 11 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
323 1910 11 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
CHEMBL1201325 1910 11 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
DB06787 1910 11 None 1 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O None
1201549 594 24 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
333 594 24 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
7601 594 24 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL1201203 594 24 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL438151 594 24 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
DB00245 594 24 None -1 20 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
43815 186896 64 3H-QNB -5 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186896 64 3H-QNB -5 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186896 64 3H-QNB -5 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
2200 3109 46 3H-NMS -11 13 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
328 3109 46 3H-NMS -11 13 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
4848 3109 46 3H-NMS -11 13 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
CHEMBL9967 3109 46 3H-NMS -11 13 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
DB00670 3109 46 3H-NMS -11 13 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 None
154825138 216012 0 3H-NMS -30 12 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
2389 3306 118 3H-QNB -22908 68 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3306 118 3H-QNB -22908 68 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3306 118 3H-QNB -22908 68 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3306 118 3H-QNB -22908 68 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3306 118 3H-QNB -22908 68 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1712 2475 43 3H-QNB -22 22 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2475 43 3H-QNB -22 22 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2475 43 3H-QNB -22 22 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2475 43 3H-QNB -22 22 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2475 43 3H-QNB -22 22 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
2028 2958 80 None -1 11 Rat 8.0 pKi = 8.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
359 2958 80 None -1 11 Rat 8.0 pKi = 8.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634 2958 80 None -1 11 Rat 8.0 pKi = 8.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
CHEMBL1231 2958 80 None -1 11 Rat 8.0 pKi = 8.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
DB01062 2958 80 None -1 11 Rat 8.0 pKi = 8.0 Binding
Affinity for rat Muscarinic acetylcholine receptor M3Affinity for rat Muscarinic acetylcholine receptor M3
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
3042 1402 35 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 1402 35 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 1402 35 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 1402 35 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 1402 35 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
2028 2958 80 None 1 11 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
359 2958 80 None 1 11 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
4634 2958 80 None 1 11 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
CHEMBL1231 2958 80 None 1 11 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
DB01062 2958 80 None 1 11 Human 8.0 pKi = 8.0 Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cellsDisplacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
Drug Central 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC None
123134663 217700 0 None -1 3 Dog 8.0 pKi = 8.0 Binding
radioligand ([3H]QNB) displacement assayradioligand ([3H]QNB) displacement assay
Drug Central 330 2 0 2 5.4 C[N@+]12CCCC[C@@H]1CCC(C2)=C(C1=CC=CS1)C1=CC=CS1 None
25897919 55622 14 None 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
657309 55622 14 None 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL1464005 55622 14 None 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL1621597 55622 14 None 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
11968014 12726 5 None -5 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 None
CHEMBL1187846 12726 5 None -5 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12 None
12057539 208018 42 None 1 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 None 1 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 None 1 21 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
367 3795 12 None -27 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
5487427 3795 12 None -27 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
8592 3795 12 None -27 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL1900528 3795 12 None -27 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL3305968 3795 12 None -27 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
CHEMBL4650755 3795 12 None -27 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
DB01409 3795 12 None -27 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 None
2784 949 13 None -6 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 None
351 949 13 None -6 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 None
366 949 13 None -6 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 None
676 949 13 None -6 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 None
CHEMBL620 949 13 None -6 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 None
DB00771 949 13 None -6 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 None
11693 1814 16 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
3494 1814 16 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
4302 1814 16 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
7459 1814 16 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
CHEMBL1201335 1814 16 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
DB00986 1814 16 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C None
25897919 55622 14 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
657309 55622 14 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL1464005 55622 14 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL1621597 55622 14 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular glandDisplacement of [3H]-NMS from Sprague-Dawley rat muscarinic M3 receptor in submandibular gland
Drug Central 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 None
10129 3297 0 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
11753673 3297 0 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
5303 3297 0 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
CHEMBL3833319 3297 0 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
DB11855 3297 0 None 1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C None
154417 23149 60 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 None
CHEMBL1331216 23149 60 None -1 5 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 None
12057539 208018 42 None -2 21 Rat 8.0 pKi = 8 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 208018 42 None -2 21 Rat 8.0 pKi = 8 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 208018 42 None -2 21 Rat 8.0 pKi = 8 Binding
Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenateAbility to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
Drug Central 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
1712 2475 43 3H-QNB -6 22 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2475 43 3H-QNB -6 22 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2475 43 3H-QNB -6 22 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2475 43 3H-QNB -6 22 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2475 43 3H-QNB -6 22 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
154825138 216012 0 3H-NMS -30 12 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
154825138 216012 0 3H-NMS -17 12 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 345 2 0 3 4.4 CC1CCCC(N1C)C=CC2C3CCCCC3CC4C2C(OC4=O)C None
135409468 2022 69 3H-QNB -32 40 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2022 69 3H-QNB -32 40 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2022 69 3H-QNB -32 40 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
4601 206724 35 3H-NMS -4 17 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 206724 35 3H-NMS -4 17 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 206724 35 3H-NMS -4 17 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
10104 3540 12 None -4 6 Human 6.9 pKi = 6.9 Binding
Binding to hM3 receptors expressed in CHO cells.Binding to hM3 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
6604866 3540 12 None -4 6 Human 6.9 pKi = 6.9 Binding
Binding to hM3 receptors expressed in CHO cells.Binding to hM3 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
CHEMBL1493369 3540 12 None -4 6 Human 6.9 pKi = 6.9 Binding
Binding to hM3 receptors expressed in CHO cells.Binding to hM3 receptors expressed in CHO cells.
Guide to Pharmacology 292 5 0 2 4.1 CN(CCC1=C([C@@H](c2ccccn2)C)c2c(C1)cccc2)C 12593665
10129 3297 0 None 1 5 Human 9.8 pKi = 9.8 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
11753673 3297 0 None 1 5 Human 9.8 pKi = 9.8 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
5303 3297 0 None 1 5 Human 9.8 pKi = 9.8 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
CHEMBL3833319 3297 0 None 1 5 Human 9.8 pKi = 9.8 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
DB11855 3297 0 None 1 5 Human 9.8 pKi = 9.8 Binding
Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM<sub>3</sub> receptor, and displacement of [<sup>3</sup>H]NMS tracer.
Guide to Pharmacology 597 10 2 6 4.8 O=C(Nc1ccccc1c1ccccc1)OC1CCN(CC1)CCN(C(=O)c1ccc(cc1)CN1CCC(CC1)C(=O)N)C 29736245
123603 880 29 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
2684 880 29 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
584 880 29 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
9658 880 29 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
CHEMBL168815 880 29 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [<sup>3</sup>H]QNB from cloned receptor.Displacement of [<sup>3</sup>H]QNB from cloned receptor.
Guide to Pharmacology 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 9399977
2293 3164 27 None -1 4 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
329 3164 27 None -1 4 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
4934 3164 27 None -1 4 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
CHEMBL1180725 3164 27 None -1 4 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
DB00782 3164 27 None -1 4 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 12049493
11434515 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 19653626
11434515 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
11519741 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 19653626
11519741 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
4484 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 19653626
4484 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
7449 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 19653626
7449 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
CHEMBL1194325 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 19653626
CHEMBL1194325 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
DB08897 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 19653626
DB08897 261 6 None -4 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 21036042
11519069 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 19317446
11519069 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
11519070 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 19317446
11519070 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
4816 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 19317446
4816 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
7354 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 19317446
7354 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
CHEMBL1187833 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 19317446
CHEMBL1187833 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
DB09076 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 19317446
DB09076 3908 3 None 1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 23435542
367 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
367 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
367 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
367 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
367 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
5487427 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
5487427 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
5487427 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
5487427 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
5487427 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
8592 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
8592 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
8592 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
8592 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
8592 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
CHEMBL1900528 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
CHEMBL1900528 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
CHEMBL1900528 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
CHEMBL1900528 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
CHEMBL1900528 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
CHEMBL3305968 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
CHEMBL3305968 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
CHEMBL3305968 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
CHEMBL3305968 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
CHEMBL3305968 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
CHEMBL4650755 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
CHEMBL4650755 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
CHEMBL4650755 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
CHEMBL4650755 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
CHEMBL4650755 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
DB01409 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
DB01409 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 19653626
DB01409 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 21036042
DB01409 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 22854200
DB01409 3795 12 None 2 8 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 8441333
316 2816 19 None -2 9 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
317 2816 19 None -2 9 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
71183 2816 19 None -2 9 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
CHEMBL3140030 2816 19 None -2 9 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
CHEMBL376897 2816 19 None -2 9 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
DB00462 2816 19 None -2 9 Human 10.4 pKi = 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 16847442
2551 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
2551 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
2551 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
298 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
298 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
298 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
488 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
488 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
488 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
CHEMBL965 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
CHEMBL965 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
CHEMBL965 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
DB00411 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10323594
DB00411 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
DB00411 791 23 None -346 11 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 9224827
2370 620 31 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
2370 620 31 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
297 620 31 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
297 620 31 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
358 620 31 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
358 620 31 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
CHEMBL1482 620 31 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
CHEMBL1482 620 31 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
DB01019 620 31 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
DB01019 620 31 None 1 5 Human 4.2 pKi = 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 9224827
187 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
187 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
187 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
294 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
294 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
294 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
65 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
65 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
65 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
8593 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
8593 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
8593 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
CHEMBL667 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
CHEMBL667 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
CHEMBL667 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
DB03128 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
DB03128 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 23798605
DB03128 255 39 None -26 9 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 9224827
303 2957 17 None -89 6 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
4629 2957 17 None -89 6 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
8595 2957 17 None -89 6 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
CHEMBL44674 2957 17 None -89 6 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 9224827
2166 3101 49 None -22 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
2166 3101 49 None -22 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
305 3101 49 None -22 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
305 3101 49 None -22 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
5910 3101 49 None -22 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
5910 3101 49 None -22 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
CHEMBL550 3101 49 None -22 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
CHEMBL550 3101 49 None -22 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
DB01085 3101 49 None -22 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 7620715
DB01085 3101 49 None -22 8 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 9224827
302 2956 25 None -309 8 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 7620715
302 2956 25 None -309 8 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 9224827
4630 2956 25 None -309 8 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 7620715
4630 2956 25 None -309 8 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 9224827
CHEMBL7634 2956 25 None -309 8 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 7620715
CHEMBL7634 2956 25 None -309 8 Human 5.3 pKi = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 9224827
2230 464 60 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
2230 464 60 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
2230 464 60 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
296 464 60 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
296 464 60 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
296 464 60 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
CHEMBL7303 464 60 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
CHEMBL7303 464 60 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
CHEMBL7303 464 60 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
DB04365 464 60 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
DB04365 464 60 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
DB04365 464 60 None -588 10 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 9224827
107867 2953 55 None -16 11 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 2704370
309 2953 55 None -16 11 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 2704370
CHEMBL17045 2953 55 None -16 11 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 2704370
24768606 3999 58 None -50 5 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 6 1 8 1.1 O=C(N1CCN(CC1)c1ccncc1)CCNS(=O)(=O)c1cccc2c1nsn2 19407080
3274 3999 58 None -50 5 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 6 1 8 1.1 O=C(N1CCN(CC1)c1ccncc1)CCNS(=O)(=O)c1cccc2c1nsn2 19407080
CHEMBL1628667 3999 58 None -50 5 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 6 1 8 1.1 O=C(N1CCN(CC1)c1ccncc1)CCNS(=O)(=O)c1cccc2c1nsn2 19407080
129786 1878 0 None -17 4 Rat 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 2 3 5 0.8 NC(=N)N1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 8813552
3276 1878 0 None -17 4 Rat 6.2 pKi = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 2 3 5 0.8 NC(=N)N1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 8813552
154734599 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
154734599 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
154734599 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
154734599 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9029489
154734599 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
327 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
327 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
327 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
327 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9029489
327 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
4108 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
4108 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
4108 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
4108 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9029489
4108 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
CHEMBL27673 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
CHEMBL27673 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
CHEMBL27673 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
CHEMBL27673 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9029489
CHEMBL27673 2486 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
2200 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
2200 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
2200 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
2200 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2704370
2200 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
2200 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
328 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
328 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
328 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
328 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2704370
328 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
328 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
4848 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
4848 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
4848 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
4848 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2704370
4848 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
4848 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
CHEMBL9967 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
CHEMBL9967 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
CHEMBL9967 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
CHEMBL9967 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2704370
CHEMBL9967 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
CHEMBL9967 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
DB00670 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 12049493
DB00670 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1994002
DB00670 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2043926
DB00670 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 2704370
DB00670 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 7925952
DB00670 3109 46 None -7 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 9113359
132947 3835 9 None -309 9 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 18595721
361 3835 9 None -309 9 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 18595721
CHEMBL265256 3835 9 None -309 9 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1124 29 4 13 10.2 CN(CCCCCCNCC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CCCCCCCCN(CCCCCCN(CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)CC(=O)n1c2ncccc2[nH]c(=O)c2c1cccc2)C 18595721
2774 3839 95 None -2 10 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 27085897
5593 3839 95 None -2 10 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 27085897
7319 3839 95 None -2 10 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 27085897
CHEMBL1200604 3839 95 None -2 10 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 27085897
DB00809 3839 95 None -2 10 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 27085897
DB01199 3839 95 None -2 10 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 27085897
324 1912 15 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1331410
324 1912 15 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1994002
324 1912 15 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 7925952
6436265 1912 15 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1331410
6436265 1912 15 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1994002
6436265 1912 15 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 7925952
CHEMBL277642 1912 15 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1331410
CHEMBL277642 1912 15 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 1994002
CHEMBL277642 1912 15 None -17 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 7925952
119357 303 49 None -16 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
3264 303 49 None -16 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
368 303 49 None -16 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
CHEMBL279453 303 49 None -16 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 9 2 5 4.5 CCCN(CC1CCCCN1CCNC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CCC 1994002
129989 450 51 None -16 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1994002
129989 450 51 None -16 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 9671109
8584 450 51 None -16 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1994002
8584 450 51 None -16 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 9671109
CHEMBL43383 450 51 None -16 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1994002
CHEMBL43383 450 51 None -16 9 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 9 1 5 4.5 CCN(CCCCC1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 9671109
3652 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
3652 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
3652 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
57 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
57 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
57 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
60809 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
60809 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
60809 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
CHEMBL21536 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
CHEMBL21536 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
CHEMBL21536 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
DB15357 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10323594
DB15357 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 36782010
DB15357 4066 79 None -3 18 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
5282426 1454 0 None -9 6 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
7549 1454 0 None -9 6 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
CHEMBL108947 1454 0 None -9 6 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 0 2 4.7 CN(CC/C=C/1\c2ccccc2SCc2c1cccc2)C 8100134
154059 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 12122494
154059 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
2457 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 12122494
2457 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
7483 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 12122494
7483 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
CHEMBL1734 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 12122494
CHEMBL1734 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
DB01591 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 12122494
DB01591 3610 51 None -1 8 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 2 0 3 3.9 O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2 20590605
180 400 56 None -23 40 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
200 400 56 None -23 40 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
2160 400 56 None -23 40 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
CHEMBL629 400 56 None -23 40 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
DB00321 400 56 None -23 40 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8100134
129140 3903 0 None -1 4 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 2043926
129140 3903 0 None -1 4 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 9671109
8583 3903 0 None -1 4 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 2043926
8583 3903 0 None -1 4 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 4.3 CN1CCC(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1c(Cl)ccc2 9671109
2705 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
2705 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
360 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
360 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
443879 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
443879 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
CHEMBL1382 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
CHEMBL1382 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
DB01036 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 20590605
DB01036 3813 64 None -1 10 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 9671109
10470 2471 7 None -11 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 24844758
1689 2471 7 None -11 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 24844758
4057 2471 7 None -11 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 24844758
CHEMBL524004 2471 7 None -11 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 24844758
DB04843 2471 7 None -11 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1CCC[N+](C1)(C)C 24844758
2028 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
2028 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
359 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
359 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
4634 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
4634 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
CHEMBL1231 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
CHEMBL1231 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
DB01062 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 20590605
DB01062 2958 80 None 1 11 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 22243489
319 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
319 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
319 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
321 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
321 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
321 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
444031 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
444031 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
444031 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
784 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
784 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
784 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
CHEMBL1346 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
CHEMBL1346 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
CHEMBL1346 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
DB00496 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 11303071
DB00496 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 20590605
DB00496 1312 44 None 2 9 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 9671109
3042 1402 35 None -1 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 1402 35 None -1 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 1402 35 None -1 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 1402 35 None -1 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 1402 35 None -1 15 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
174174 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
174174 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
174174 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
174174 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
260 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
260 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
260 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
260 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
320 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
320 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
320 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
320 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
CHEMBL517712 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
CHEMBL517712 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
CHEMBL517712 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
CHEMBL517712 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
DB00572 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 11303071
DB00572 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12049493
DB00572 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 27085897
DB00572 521 49 None -2 14 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 3443095
1734 116 10 None -2 13 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1325587
307 116 10 None -2 13 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1325587
CHEMBL168067 116 10 None -2 13 Rat 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1325587
1734 116 10 None 1 13 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1994002
307 116 10 None 1 13 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1994002
CHEMBL168067 116 10 None 1 13 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 1994002
3000322 3536 38 None 1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 12049493
3000322 3536 38 None 1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 1346637
330 3536 38 None 1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 12049493
330 3536 38 None 1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 1346637
CHEMBL569713 3536 38 None 1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 12049493
CHEMBL569713 3536 38 None 1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 1346637
DB00747 3536 38 None 1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 12049493
DB00747 3536 38 None 1 6 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 1346637
325 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
325 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 16847442
325 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 19653626
3746 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
3746 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 16847442
3746 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 19653626
657308 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
657308 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 16847442
657308 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 19653626
CHEMBL1615433 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
CHEMBL1615433 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 16847442
CHEMBL1615433 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 19653626
DB00332 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 11303071
DB00332 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 16847442
DB00332 2049 0 None -1 9 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 332 5 1 3 2.9 OCC(c1ccccc1)C(=O)OC1CC2CCC(C1)[N+]2(C)C(C)C 19653626
2784 949 13 None -6 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 16847442
351 949 13 None -6 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 16847442
366 949 13 None -6 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 16847442
676 949 13 None -6 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 16847442
CHEMBL620 949 13 None -6 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 16847442
DB00771 949 13 None -6 3 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 16847442
8586 300 0 None 2 4 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 336 5 2 3 1.8 CN(C(=O)C(c1ccccc1)(c1ccccc1)O)C[C@@H]1[C@H]2[C@@H]1CNC2 20590605
9862598 300 0 None 2 4 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 336 5 2 3 1.8 CN(C(=O)C(c1ccccc1)(c1ccccc1)O)C[C@@H]1[C@H]2[C@@H]1CNC2 20590605
42519285 2560 15 None -60 5 Human 4.5 pKi > 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 7 0 6 3.7 CN(C(=O)c1noc(c1)COc1cccc(c1)C(=O)C)[C@H](c1ccccn1)C 24692176
8591 2560 15 None -60 5 Human 4.5 pKi > 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 7 0 6 3.7 CN(C(=O)c1noc(c1)COc1cccc(c1)C(=O)C)[C@H](c1ccccn1)C 24692176
CHEMBL3185781 2560 15 None -60 5 Human 4.5 pKi > 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 379 7 0 6 3.7 CN(C(=O)c1noc(c1)COc1cccc(c1)C(=O)C)[C@H](c1ccccn1)C 24692176
314 2673 0 None -1122018 5 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10799315
313 2672 0 None -407 6 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7925952
134 2497 24 None -134 68 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2497 24 None -134 68 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2497 24 None -134 68 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2497 24 None -134 68 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2497 24 None -134 68 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
46780481 107504 20 None -776 54 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107504 20 None -776 54 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107504 20 None -776 54 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107504 20 None -776 54 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
3337 206344 27 None -158 41 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206344 27 None -158 41 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206344 27 None -158 41 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206344 27 None -158 41 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206344 27 None -158 41 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3012003 216119 0 None -1 12 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 311 5 0 3 3.8 CN1CCC(C(C1)COC2=CC=C(C=C2)OC)C3=CC=CC=C3 None
11976 917 59 None -12 24 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 917 59 None -12 24 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 917 59 None -12 24 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 917 59 None -12 24 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
2895 203569 41 None -1 8 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
CHEMBL669 203569 41 None -1 8 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
4066 204603 78 None 1 7 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
CHEMBL73451 204603 78 None 1 7 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 None
10938 1689 0 None -1 4 Human 4.1 pKi None 4.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
299 1689 0 None -1 4 Human 4.1 pKi None 4.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
3256 1689 0 None -1 4 Human 4.1 pKi None 4.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
CHEMBL2110739 1689 0 None -1 4 Human 4.1 pKi None 4.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 140 2 0 1 1.5 C[N+](Cc1ccco1)(C)C 9224827
2551 791 23 None -54 11 Rat 4.2 pKi None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
298 791 23 None -54 11 Rat 4.2 pKi None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
488 791 23 None -54 11 Rat 4.2 pKi None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
CHEMBL965 791 23 None -54 11 Rat 4.2 pKi None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
DB00411 791 23 None -54 11 Rat 4.2 pKi None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 12235229
300 2493 15 None -3 6 Human 4.6 pKi None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 9224827
4141 2493 15 None -3 6 Human 4.6 pKi None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 9224827
CHEMBL92387 2493 15 None -3 6 Human 4.6 pKi None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 1 1.8 Cc1ccc(o1)C[N+](C)(C)C 9224827
301 2517 19 None -7 5 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10323594
9571002 2517 19 None -7 5 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10323594
CHEMBL151938 2517 19 None -7 5 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10323594
290 2456 6 None -7 7 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7620715
4022 2456 6 None -7 7 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7620715
5926 2456 6 None -7 7 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7620715
CHEMBL40554 2456 6 None -7 7 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7620715
CHEMBL74300 2456 6 None -7 7 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 7620715
187 255 39 None -34 9 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
294 255 39 None -34 9 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
65 255 39 None -34 9 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
8593 255 39 None -34 9 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
CHEMBL667 255 39 None -34 9 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
DB03128 255 39 None -34 9 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 12235229
2229 463 22 None -3 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 9224827
295 463 22 None -3 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 9224827
CHEMBL128365 463 22 None -3 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 0 3 0.4 CN1CC(=CCC1)C(=O)OCC#C 9224827
22991950 2314 0 None 1 6 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 7 2 2 5.9 OC(C[N+](C)(C)C)CCCC(C1CCC2C1(C)CCC1C2CCC2C1(C)CCC(C2)O)C 12235229
22991950 2314 0 None -1 6 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 7 2 2 5.9 OC(C[N+](C)(C)C)CCCC(C1CCC2C1(C)CCC1C2CCC2C1(C)CCC(C2)O)C 12235229
326 2314 0 None 1 6 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 7 2 2 5.9 OC(C[N+](C)(C)C)CCCC(C1CCC2C1(C)CCC1C2CCC2C1(C)CCC(C2)O)C 12235229
326 2314 0 None -1 6 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 7 2 2 5.9 OC(C[N+](C)(C)C)CCCC(C1CCC2C1(C)CCC1C2CCC2C1(C)CCC(C2)O)C 12235229
107867 2953 55 None -12 11 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1325587
309 2953 55 None -12 11 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1325587
CHEMBL17045 2953 55 None -12 11 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 421 6 1 5 3.5 CCN(CC1CCCCN1CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2)CC 1325587
2200 3109 46 None -11 13 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
328 3109 46 None -11 13 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
4848 3109 46 None -11 13 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
CHEMBL9967 3109 46 None -11 13 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
DB00670 3109 46 None -11 13 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 1325587
306 3430 21 None -4 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
3536 3430 21 None -4 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
53930639 3430 21 None -4 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
9577995 3430 21 None -4 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
CHEMBL134641 3430 21 None -4 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10323594
10426487 2821 7 None -2 5 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 11504829
291 2821 7 None -2 5 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 11504829
CHEMBL99521 2821 7 None -2 5 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 11504829
308 2047 23 None -1 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 12049493
308 2047 23 None -1 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 8759038
3603 2047 23 None -1 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 12049493
3603 2047 23 None -1 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 8759038
CHEMBL1256682 2047 23 None -1 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 12049493
CHEMBL1256682 2047 23 None -1 9 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 8759038
124226 1908 0 None -1 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 2 4.7 OC(c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
322 1908 0 None -1 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 2 4.7 OC(c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
310 1909 0 None -3 11 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
310 1909 0 None -3 11 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 8759038
3602 1909 0 None -3 11 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
3602 1909 0 None -3 11 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 8759038
CHEMBL3545990 1909 0 None -3 11 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 2704370
CHEMBL3545990 1909 0 None -3 11 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 6 1 2 4.0 O[Si](c1ccccc1)(C1CCCCC1)CCCN1CCCCC1 8759038
308 2047 23 None 1 9 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 1325587
3603 2047 23 None 1 9 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 1325587
CHEMBL1256682 2047 23 None 1 9 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 6 1 2 4.2 Fc1ccc(cc1)[Si](C1CCCCC1)(CCCN1CCCCC1)O 1325587
293 2823 0 None -3 5 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1cccc(c1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
9985526 2823 0 None -3 5 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1cccc(c1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
10062394 3025 1 None -3 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 6 0 5 3.5 CCCCCSc1nsnc1C1=CCCN(C1)C 9224827
304 3025 1 None -3 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 6 0 5 3.5 CCCCCSc1nsnc1C1=CCCN(C1)C 9224827
CHEMBL130715 3025 1 None -3 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 6 0 5 3.5 CCCCCSc1nsnc1C1=CCCN(C1)C 9224827
11757797 2822 0 None -63 5 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccc(cc1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
292 2822 0 None -63 5 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 572 6 0 10 3.9 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccc(cc1)C#CCOc1nsnc1C1CN2CCC1CC2 11504829
1371 1910 11 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
24199 1910 11 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
323 1910 11 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
CHEMBL1201325 1910 11 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
DB06787 1910 11 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 2704370
130169 3578 0 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O 2704370
331 3578 0 None 1 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 2 2.1 C[N+]1(C)CCN(CC1)C[Si](c1ccccc1)(C1CCCCC1)O 2704370
174174 521 49 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12235229
174174 521 49 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
260 521 49 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12235229
260 521 49 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
320 521 49 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12235229
320 521 49 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
CHEMBL517712 521 49 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12235229
CHEMBL517712 521 49 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587
DB00572 521 49 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 12235229
DB00572 521 49 None -1 14 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 1325587