Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
9815409 19136 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 19136 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 19136 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 84101 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 84101 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 18749 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 18749 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 18749 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 10869 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 10869 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 10869 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 10869 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 10869 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 17922 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 17922 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 17922 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 192067 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 192067 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 193842 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 193842 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 10229 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 10229 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 10229 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 10229 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 10229 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 10869 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 10869 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 10869 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 10869 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 10869 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 7581 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 7581 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 7581 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 7581 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 7581 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 9275 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 9275 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 9275 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 9275 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 9275 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 7253 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 7253 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 7253 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 7253 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 20726 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 20726 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 20726 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 7581 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 7581 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 7581 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 7581 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 7581 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 61188 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 61188 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 61188 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 22850 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 22850 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 22878 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 22878 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 7581 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 7581 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 7581 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 7581 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 7581 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 24526 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 24526 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 24526 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 24526 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 7581 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 7581 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 7581 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 7581 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 7581 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 184371 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 184371 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 20482 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 20482 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 20482 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 212877 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 212877 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 22876 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 22876 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 113116 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 113116 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 184893 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 184893 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 19925 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 19925 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 19925 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 19925 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 19966 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 19966 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 19966 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 19966 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 7581 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 7581 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 7581 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 7581 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 7581 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 184331 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 184331 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 22852 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 22852 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 22875 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 22875 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7581 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 7581 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 7581 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 7581 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 7581 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 9354 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 9354 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 9354 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 195449 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 195449 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 195449 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 195449 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 7581 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 7581 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 7581 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 7581 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 7581 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 22826 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 22826 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 22877 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 22877 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 22826 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 22826 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 10869 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 10869 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 10869 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 10869 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 10869 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 85181 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 85181 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 13833 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 13833 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 18625 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 18625 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 18625 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 23328 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 23328 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 209886 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 209886 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 107313 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 107313 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 107313 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 9354 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 9354 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 9354 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 22851 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 22851 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 22896 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 22896 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 22895 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 22895 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 22898 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 22898 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 87232 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 87232 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 87234 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 87234 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 184071 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 184071 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 102780 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 102780 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 102780 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 7581 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 7581 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 7581 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 7581 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 7581 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 7581 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 7581 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 7581 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 7581 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 7581 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 19717 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 19717 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 19717 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 19717 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 7581 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 7581 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 7581 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 7581 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 7581 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 18623 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 18623 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 18623 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 18625 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 18625 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 18625 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 18760 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 18760 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 18760 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 7024 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 7024 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 7024 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 47186 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 47186 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 185041 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 185041 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 185041 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 185033 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 185033 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 185033 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 184371 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 184371 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 22849 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 22849 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 22897 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 22897 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 10795 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 10795 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 10795 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 186932 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 186932 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 10795 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 10795 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 10795 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 10795 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 10795 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 10795 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 8816 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 8816 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 8816 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 34092 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 34092 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 22827 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 22827 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 22874 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 22874 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 113839 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 113839 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 127494 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 127494 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 127108 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 127108 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 184071 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 184071 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 7581 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 7581 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 7581 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 7581 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 7581 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 65504 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 65504 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 212425 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 212425 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 103263 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 103263 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 113255 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 113255 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 113255 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 221094 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 221098 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 221094 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 221805 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 195671 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 195671 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 195671 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 221098 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 113288 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 113288 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 113288 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 194082 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 194082 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 194141 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 194141 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 199503 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 199503 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 192759 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 192759 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 195870 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 195870 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 195870 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 221246 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 90693 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 90693 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 110278 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 110278 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 194091 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 194091 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 179536 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 179536 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 179537 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 179537 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 194499 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 194499 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 182422 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 182422 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 169262 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 169262 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 92800 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 92800 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 92800 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 92800 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 110274 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 110274 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 110280 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 110280 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 113276 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 113276 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 113276 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 113280 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 113280 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 113280 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 113242 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 113242 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 113242 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 169061 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 169061 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 169121 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 169121 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 113263 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 113263 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 113263 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 110270 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 110270 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 110271 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 110271 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 176836 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 176836 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 176836 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 195701 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 195701 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 195701 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 221224 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 19393 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 19393 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 19393 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 179496 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 179496 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 179496 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 193991 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 193991 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 199929 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 199929 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 180343 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 180343 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 180343 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 186419 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 186419 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 90782 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 90782 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 19407 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 19407 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 19407 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 169040 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 169040 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 92821 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 92821 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 92821 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 92821 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 110026 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 110026 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 110029 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 110029 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 110281 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 110281 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 113300 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 113300 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 113300 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 90705 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 90705 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 110025 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 110025 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 200197 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 200197 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 176222 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 176222 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 176222 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 176573 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 176573 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 177097 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 177097 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 177097 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 185527 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 185527 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 185527 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 190640 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 190640 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 195150 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 195150 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 195150 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 200197 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 200197 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 113298 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 113298 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 113298 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 179366 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 179366 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 90711 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 90711 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 195191 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 195191 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 194428 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 194428 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 195684 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 195684 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 113261 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 113261 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 113261 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 113246 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 113246 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 113246 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 19529 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 19529 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 19529 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 110027 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 110027 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 195544 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 195544 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 193986 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 193986 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 194380 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 194380 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 190457 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 190457 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 195544 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 195544 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 197337 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 197337 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 7384 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 7384 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 7384 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 7384 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 7384 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 7384 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 221220 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 221307 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 221805 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 110168 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 110168 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 110168 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 110168 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 90691 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 90691 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 193981 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 193981 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 194381 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 194381 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 194412 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 194412 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 194413 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 194413 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 195160 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 195160 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 195172 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 195172 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 113278 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 113278 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 113278 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 113283 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 113283 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 113283 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 113274 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 113274 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 113274 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 110264 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 110264 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 110155 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 110155 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 110155 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 110155 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 113299 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 113299 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 113299 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 110272 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 110272 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 110277 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 110277 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 19396 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 19396 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 19396 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 90706 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 90706 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 113247 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 113247 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 113247 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 199852 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 199852 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 169285 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 169285 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 110269 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 110269 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 199852 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 199852 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 90712 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 90712 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 104541 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 104541 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 113262 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 113262 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 113262 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 179425 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 179425 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 179425 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 185803 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 185803 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 189930 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 189930 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 196756 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 196756 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 194227 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 194227 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 194306 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 194306 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 194388 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 194388 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 182072 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 182072 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 193980 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 193980 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 193980 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 200069 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 200069 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 198620 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 198620 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 81054 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 81054 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 110273 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 110273 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 110265 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 110265 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 90695 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 90695 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 110173 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 110173 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 110173 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 110173 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 130883 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 130883 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 130883 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 130883 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 110176 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 110176 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 110176 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 110176 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 113271 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 113271 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 113271 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 113291 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 113291 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 113291 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 221307 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 194432 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 194432 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 19391 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 19391 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 19391 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 194109 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 194109 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 199908 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 199908 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 195156 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 195156 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 195844 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 195844 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 195844 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 101892 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 101892 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 194044 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 194044 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 194092 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 194092 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 194307 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 194307 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 194396 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 194396 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 194431 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 194431 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 193299 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 193299 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 195545 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 195545 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 100043 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 100043 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 194266 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 194266 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 113240 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 113240 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 113240 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 81056 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 81056 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 168794 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 168794 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 90710 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 90710 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 113237 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 113237 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 113237 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 115742 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 115742 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 19517 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 19517 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 19517 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 164625 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 164625 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 113281 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 113281 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 113281 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 14663 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 14663 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 162594 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 162594 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 194040 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 194040 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 195022 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 195022 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 195022 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 19372 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 19372 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 19372 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 90699 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 90699 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 179467 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 179467 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 194268 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 194268 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 199932 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 199932 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 113268 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 113268 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 113268 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 165752 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 165752 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 113284 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 113284 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 113284 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 130888 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 130888 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 90781 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 90781 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 130887 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 130887 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 113254 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 113254 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 113254 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 14666 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 14666 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 110276 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 110276 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 14665 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 14665 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 90709 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 90709 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 90701 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 90701 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 194142 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 194142 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 192760 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 192760 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 221220 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 221549 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 194116 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 194116 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 194378 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 194378 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 194461 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 194461 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 195411 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 195411 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 195411 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 198533 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 198533 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 189531 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 189531 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 90694 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 90694 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 194041 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 194041 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 194390 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 194390 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 194414 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 194414 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 194498 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 194498 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 200091 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 200091 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 179511 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 179511 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 195764 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 195764 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 187622 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 187622 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 194088 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 194088 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 90700 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 90700 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 130890 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 130890 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 130888 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 130888 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 199852 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 199852 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 199852 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 199852 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 189531 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 189531 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 113260 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 113260 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 113260 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 15036 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 15036 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 110275 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 110275 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 130887 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 130887 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 90703 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 90703 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 130890 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 130890 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 90708 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 90708 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 199494 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 199494 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 179260 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 179260 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 179260 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 179508 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 179508 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 179508 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 195558 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 195558 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 195558 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 199339 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 199339 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 113253 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 113253 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 113253 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 165763 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 165763 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 221549 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 194086 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 194086 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 200018 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 200018 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 194389 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 194389 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 194429 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 194429 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 110154 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 110154 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 113269 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 113269 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 113269 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 113243 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 113243 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 113243 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 113256 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 113256 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 113256 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 165795 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 165795 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 90702 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 90702 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 110178 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 110178 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 110178 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 110178 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 110279 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 110279 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 179517 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 179517 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 179517 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 190639 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 190639 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 90704 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 90704 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 165810 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 165810 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 101830 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 101830 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 113285 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 113285 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 113285 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 110266 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 110266 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 113270 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 113270 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 113270 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 110263 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 110263 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 168907 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 168907 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 110268 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 110268 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 163656 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 163656 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 194053 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 194053 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 194087 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 194087 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 194463 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 194463 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 221224 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 194379 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 194379 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 196195 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 196195 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 194417 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 194417 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 90707 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 90707 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 15263 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 15263 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 92849 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 92849 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 92849 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 92849 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 113241 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 113241 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 113241 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 19339 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 19339 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 19339 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 169781 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 169781 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 113239 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 113239 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 113239 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 19402 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 19402 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 19402 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 169731 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 169731 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 113286 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 113286 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 113286 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 110167 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 110167 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 199381 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 199381 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 199381 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 199381 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 208217 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 208217 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 208217 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 85161 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 85161 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 85161 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 85161 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 85161 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 85161 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 179927 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 179927 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 179927 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 19390 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 19390 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 19390 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 195176 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 195176 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 195176 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 81230 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 81230 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 81230 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 10711 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 10711 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 10711 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 10711 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 10711 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 10711 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 199412 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 199412 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 19389 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 19389 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 19389 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 19397 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 19397 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 19397 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 19533 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 19533 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 19533 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 81254 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 81254 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 81254 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 194130 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 194130 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 194131 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 194131 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 113250 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 113250 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 113250 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 113266 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 113266 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 113266 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 113267 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 113267 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 113267 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 110160 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 110160 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 19519 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 19519 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 19519 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 19525 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 19525 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 19525 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 195727 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 195727 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 19516 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 19516 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 19516 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 177707 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 177707 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 177707 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 194496 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 194496 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 81240 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 81240 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 81240 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 110031 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 110031 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 113257 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 113257 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 113257 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 113302 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 113302 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 113302 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 19337 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 19337 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 19337 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 85161 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 85161 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 85161 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 179463 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 179463 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 179463 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 195567 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 195567 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 195567 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 195833 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 195833 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 195833 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 113301 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 113301 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 113301 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 19535 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 19535 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 19535 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 179363 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 179363 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 179363 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 194497 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 194497 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 195091 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 195091 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 195091 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 179363 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 179363 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 179363 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 193995 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 193995 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 193995 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 193995 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 194144 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 194144 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 194144 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 194144 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 113251 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 113251 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 113251 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 113273 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 113273 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 113273 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 194397 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 194397 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 87550 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 87550 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 194156 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 194156 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 19392 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 19392 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 19392 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 199934 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 199934 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 110160 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 110160 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 10711 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 10711 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 10711 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 10711 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 10711 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 10711 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 19388 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 19388 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 19388 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 19399 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 19399 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 19399 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 19526 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 19526 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 19526 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 113252 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 113252 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 113252 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 113252 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 113252 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 113252 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 19377 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 19377 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 19377 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 19400 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 19400 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 19400 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 113238 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 113238 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 113238 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 199856 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 199856 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 178420 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 178420 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 178420 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 195835 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 195835 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 195835 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 113277 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 113277 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 113277 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 19521 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 19521 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 19521 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 113305 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 113305 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 113305 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 113302 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 113302 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 113302 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 19534 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 19534 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 19534 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 113275 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 113275 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 113275 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 113304 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 113304 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 113304 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 113303 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 113303 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 113303 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 19508 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 19508 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 19508 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 179949 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 179949 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 179949 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 195747 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 195747 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 195747 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 113280 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 113280 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 113280 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 19402 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 19402 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 19402 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 179363 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 179363 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 179363 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 110028 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 110028 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 110167 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 110167 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 113244 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 113244 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 113244 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 110167 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 110167 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 113259 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 113259 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 113259 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 19396 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 19396 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 19396 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 19398 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 19398 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 19398 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 194143 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 194143 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 194143 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 194251 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 194251 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 192080 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 192080 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 192080 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 110179 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 110179 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 113259 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 113259 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 113259 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 110179 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 110179 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 19407 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 19407 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 19407 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 113287 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 113287 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 113287 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 113288 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 113288 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 113288 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 74702 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 74702 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 74706 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 74706 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 74711 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 74711 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 62426 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 62426 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 62426 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 62426 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 74710 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 74710 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 74705 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 74705 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 74716 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 74716 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 74700 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 74700 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 74719 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 74719 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 74703 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 74703 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 74704 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 74704 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 74714 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 74714 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 74717 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 74717 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 74720 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 74720 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 74712 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 74712 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 74707 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 74707 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 74701 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 74701 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 74715 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 74715 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 145210 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 145210 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 74709 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 74709 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 152136 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 152136 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 158950 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 158950 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 145371 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 145371 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 145246 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 145246 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 159740 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 159740 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 155656 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 155656 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 156784 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 156784 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 74713 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 74713 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 74708 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 74708 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 74699 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 74699 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 160768 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 160768 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 160978 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 160978 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 145319 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 145319 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 152024 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 152024 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 145324 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 145324 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 151122 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 151122 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 154954 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 154954 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 82803 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 82803 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 155697 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 155697 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 149811 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 149811 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 159163 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 159163 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 150332 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 150332 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 157424 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 157424 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 145257 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 145257 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 150622 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 150622 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 158508 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 158508 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 150152 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 150152 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 158344 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 158344 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 74718 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 74718 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 112186 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 112186 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 156533 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 156533 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 103414 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 103414 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 84101 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 84101 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 9275 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 9275 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 9275 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 9275 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 9275 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 9897 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 9897 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 9897 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 9897 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 9897 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 7670 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 7670 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 7670 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 7670 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 7670 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 222742 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 10795 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 10795 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 10795 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 9275 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 9275 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 9275 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 9275 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 9275 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 9275 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 9275 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 9275 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 9275 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 9275 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 7040 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 7040 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 7039 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 7039 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 224479 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 224486 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 10409 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 10409 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 10409 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 10409 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 10409 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 224523 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 (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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367 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 62426 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 62426 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 62426 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 62426 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 7739 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 7739 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 7739 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 7739 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 7739 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 7739 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 10335 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 10335 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 10335 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 10335 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 7293 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 7293 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 7293 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 7293 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 7293 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 10879 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 10879 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 10879 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 10879 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 10879 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 143746 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 143746 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 143746 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 9869 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 9869 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 9869 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 9869 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 9869 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 22348 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 22348 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 22348 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 118358 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 118358 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 212306 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 212306 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 212306 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 64181 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 64181 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 130868 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 130868 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 8196 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 8196 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 8196 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 8196 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 8196 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 7736 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 7736 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 7736 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 7736 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 7736 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 9956 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 9956 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 9956 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 9956 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 9956 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 7383 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 7383 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 7383 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 7383 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 7383 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 9947 58 None -21 31 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 9947 58 None -21 31 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 9947 58 None -21 31 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 9947 58 None -21 31 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 9947 58 None -21 31 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 106099 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 106099 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 21265 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 21265 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 21265 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 21265 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 21265 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 21265 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 37995 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 37995 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 69259 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 69259 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 69259 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 84948 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 84948 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 214020 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 214020 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 213013 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 213013 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 14657 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 14657 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 14657 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 11173 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 11173 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 9127 53 None -19 44 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 9127 53 None -19 44 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 9127 53 None -19 44 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 9127 53 None -19 44 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 9127 53 None -19 44 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 85174 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 85174 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 7725 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 7725 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 7725 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 7725 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 7725 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 16197 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 16197 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 89183 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 89183 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 104849 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 104849 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 7706 68 None -18 72 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 7706 68 None -18 72 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 7706 68 None -18 72 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 7706 68 None -18 72 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 7706 68 None -18 72 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 22066 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 22066 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 203265 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 203265 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 201505 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 201505 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 7741 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 7741 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 7741 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 7741 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 7741 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 8411 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 8411 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 8411 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 8411 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 8411 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 41835 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 41835 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 41835 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 11072 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 11072 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 11072 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 185571 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 185571 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 18032 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 18032 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 208912 58 None - 4 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 208912 58 None - 4 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8963 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 8963 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 8963 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 8963 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 8963 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 21242 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 21242 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 8214 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 8214 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 8214 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 8214 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 8214 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 8214 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 212750 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 212750 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 9121 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 9121 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 9121 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 9121 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 9121 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 103323 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 103323 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 62194 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 62194 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 10614 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 10614 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 10614 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 10614 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 10614 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 21271 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 21271 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 9310 43 None -22 56 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 9310 43 None -22 56 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 9310 43 None -22 56 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 9310 43 None -22 56 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 9310 43 None -22 56 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 9905 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 9905 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 9905 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 9905 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 9905 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 109507 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 109507 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 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1213 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
2725 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
33036 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
4411 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
616 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
6976 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
716121 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1201353 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1554789 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL505 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB01114 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB13679 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
47472 26209 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 26209 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 64180 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 64180 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 201463 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 201463 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 10362 83 None -239 48 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 10362 83 None -239 48 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 10362 83 None -239 48 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 10362 83 None -239 48 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 10362 83 None -239 48 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 34760 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 34760 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 100709 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 100709 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 210358 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 210358 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 127026 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 127026 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 21192 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 21192 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 7384 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 7384 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 7384 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 7384 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 7384 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 7384 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 7189 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 7189 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 7189 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 7189 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 7189 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 109635 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 109635 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 161635 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 161635 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 9538 19 None - 18 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 9538 19 None - 18 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 9538 19 None - 18 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 19768 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 19768 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 42104 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 42104 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 42104 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 84915 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 211184 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 211184 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 211184 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 201316 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 7191 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 7191 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 7191 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 7191 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 7191 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 21264 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 21264 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 21264 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 21264 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 9957 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 9957 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 9957 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 9957 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 9957 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 10925 61 None -144 53 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 10925 61 None -144 53 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 10925 61 None -144 53 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 10925 61 None -144 53 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 10925 61 None -144 53 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 210371 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 210371 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 36049 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 36049 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 36049 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 19302 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 19302 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 23421 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 23421 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 23421 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 9688 112 None -27 65 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 9688 112 None -27 65 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 9688 112 None -27 65 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 9688 112 None -27 65 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 10640 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 10640 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 10640 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 10640 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 10640 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 10640 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 63041 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 63041 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 15929 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 15929 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 29953 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 29953 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 21270 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 21270 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 48495 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 48495 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 18620 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 18620 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 18620 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 18620 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 193699 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 193699 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 193699 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 213174 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 213174 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 21247 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 21247 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 7745 93 None -10 90 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 7745 93 None -10 90 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 7745 93 None -10 90 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 7745 93 None -10 90 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 7745 93 None -10 90 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 203214 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 203214 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 10641 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 10641 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 10641 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 10641 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 10641 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 9641 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 9641 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 9641 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 9641 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 9641 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 21183 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 21183 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 25757 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 25757 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 106089 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 106089 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 8439 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 8439 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 8439 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 8439 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 8439 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 96369 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 96369 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 74383 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 74383 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 10335 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 10335 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 10335 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 10335 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 24764 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 24764 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 44182 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 44182 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 8171 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 8171 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 8171 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 8171 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 8171 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 10632 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 10632 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 10632 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 10632 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 10632 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 10632 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 24730 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 24730 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 212050 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 212050 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 212050 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 212050 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 212050 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 212050 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 212050 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 8794 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 8794 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 8794 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 8794 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 8794 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 74176 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 74176 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 74176 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 185007 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 185007 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 8445 49 None - 32 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 8445 49 None - 32 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 8445 49 None - 32 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 8445 49 None - 32 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 8445 49 None - 32 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 12490 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 12490 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 19386 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 19386 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 10577 58 None -8 54 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 10577 58 None -8 54 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 10577 58 None -8 54 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 10577 58 None -8 54 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 10577 58 None -8 54 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 74345 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 74345 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 10030 77 None -81 62 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 10030 77 None -81 62 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 10030 77 None -81 62 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 10030 77 None -81 62 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 10030 77 None -81 62 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 69957 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 69957 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 174297 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 174297 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 174297 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 211405 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 211405 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 119361 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 119361 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 7450 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 7450 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 7450 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 7450 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 7450 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 8437 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 8437 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 8437 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 8437 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 8437 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 210398 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 210398 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 58444 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 58444 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 7253 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 7253 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 7253 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 7253 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 24526 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 24526 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 24526 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 24526 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 167755 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 167755 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 167755 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 213843 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 213843 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 167755 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 167755 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 167755 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 17843 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 17843 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 17843 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 210728 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 210728 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 18716 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 18716 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 18716 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 109562 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 109562 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 9897 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 9897 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 9897 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 9897 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 9897 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 18725 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 18725 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 18725 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 201392 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 201392 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 201039 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 9752 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 9752 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 9752 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 9752 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 17838 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 17838 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 17838 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 185033 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 185033 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 185033 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 185041 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 185041 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 185041 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 17840 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 17840 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 17840 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 200519 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 7581 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 7581 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 7581 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 7581 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 7581 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 9751 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 9751 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 9751 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 7581 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 7581 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 7581 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 7581 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 7581 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7581 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 7581 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 7581 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 7581 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 7581 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 10409 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 10409 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 10409 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 10409 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 10409 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 184331 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 184331 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 184371 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 184371 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 184893 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 184893 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 201409 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 201409 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 104032 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 104032 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 201441 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 201441 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 7253 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 7253 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 7253 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 7253 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 17841 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 17841 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 17841 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 167799 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 167799 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 167799 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 184071 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 184071 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 17847 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 17847 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 17847 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 210727 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 210727 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 109385 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 109385 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 10795 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 10795 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 10795 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 7581 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 7581 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 7581 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 7581 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 7581 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 104936 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 104936 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 104936 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 78406 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 78406 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 78406 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 110504 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 110504 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 75522 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 75522 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 75923 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 75923 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 110412 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 110412 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 110416 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 110416 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 75521 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 75521 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 75536 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 75536 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 75546 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 75546 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 110506 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 110506 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 110513 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 110513 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 110517 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 110517 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 75528 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 75528 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 75548 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 75548 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 110502 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 110502 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 110507 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 110507 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 110512 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 110512 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 75556 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 75556 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 75611 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 75611 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 75919 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 75919 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 110422 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 110422 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 110494 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 110494 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 110497 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 110497 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 75530 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 75530 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 75552 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 75552 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 75557 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 75557 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 75930 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 75930 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 110419 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 110419 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 110516 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 110516 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 75520 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 75520 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 75524 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 75524 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 75529 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 75529 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 75609 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 75609 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 75612 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 75612 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 75910 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 75910 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 110413 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 110413 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 110421 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 110421 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 110435 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 110435 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 110440 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 110440 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 110441 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 110441 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 110498 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 110498 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 110515 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 110515 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 20683 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 20683 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 20683 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 75523 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 75523 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 75527 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 75527 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 75538 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 75538 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 75551 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 75551 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 75553 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 75553 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 75554 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 75554 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 75555 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 75555 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 75608 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 75608 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 75610 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 75610 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 75613 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 75613 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 110417 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 110417 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 110437 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 110437 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 110491 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 110491 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 69904 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 69904 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 69904 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 20798 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 20798 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 20798 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 151218 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 151218 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 154773 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 154773 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 202116 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 202116 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 152592 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 152592 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 20396 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 20396 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 20396 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 20672 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 20672 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 20672 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 20673 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 20673 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 20673 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 136078 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 136078 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 136079 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 136079 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 75539 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 75539 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 75616 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 75616 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 75912 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 75912 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 110418 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 110418 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 110442 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 110442 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 110447 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 110447 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 110499 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 110499 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 110505 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 110505 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 20800 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 20800 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 20800 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 69901 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 69901 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 69901 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 69908 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 69908 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 69908 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 150558 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 150558 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 152391 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 152391 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 136080 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 136080 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 6904 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 6904 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 6904 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 20773 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 20773 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 20773 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 203472 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 203472 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 75532 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 75532 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 75535 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 75535 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 75543 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 75543 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 75614 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 75614 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 110503 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 110503 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 20395 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 20395 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 20395 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 20390 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 20390 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 20390 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 203160 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 203160 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 75537 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 75537 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 75615 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 75615 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 110424 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 110424 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 110449 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 110449 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 110500 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 110500 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 149322 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 149322 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 151085 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 151085 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 158106 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 158106 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 158407 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 158407 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 6904 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 6904 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 6904 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 6904 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 6904 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 6904 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 202427 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 202427 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 6904 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 6904 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 6904 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 20564 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 20564 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 20564 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 20801 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 20801 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 20801 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 69902 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 69902 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 69902 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 151500 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 151500 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 75550 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 75550 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 110415 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 110415 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 110443 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 110443 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 6904 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 6904 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 6904 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 20787 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 20787 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 20787 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 6904 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 6904 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 6904 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 69113 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 69113 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 69899 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 69899 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 69899 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 69903 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 69903 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 69903 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 69912 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 69912 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 69912 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 69913 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 69913 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 69913 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 20785 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 20785 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 20785 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 149459 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 149459 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 158011 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 158011 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 20398 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 20398 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 20398 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 75540 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 75540 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 75547 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 75547 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 75929 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 75929 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 110439 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 110439 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 110444 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 110444 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 110493 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 110493 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 127654 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 127654 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 127654 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 127656 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 127656 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 127656 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 127657 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 127657 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 127657 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 202334 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 202334 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 155505 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 155505 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 20789 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 20789 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 20789 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 168346 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 168346 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 201847 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 201847 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 75549 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 75549 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 75913 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 75913 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 75914 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 75914 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 110445 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 110445 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 110448 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 110448 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 110451 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 110451 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 110492 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 110492 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 127664 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 127664 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 127664 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 69900 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 69900 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 69900 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 69911 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 69911 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 69911 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 151804 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 151804 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 69914 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 69914 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 69914 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 202662 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 202662 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 203351 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 203351 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 20784 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 20784 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 20784 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 69114 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 69114 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 69906 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 69906 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 69906 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 75544 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 75544 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 75607 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 75607 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 75916 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 75916 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 75925 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 75925 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 110414 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 110414 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 110450 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 110450 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 153439 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 153439 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 158252 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 158252 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 20791 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 20791 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 20791 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 20792 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 20792 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 20792 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 124556 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 124556 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 160092 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 160092 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 21255 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 21255 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 21255 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 68915 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 68915 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 69905 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 69905 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 69905 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 25949 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 25949 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 75533 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 75533 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 75542 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 75542 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 75606 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 75606 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 75915 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 75915 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 7384 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 7384 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 7384 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 7384 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 7384 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 7384 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 150771 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 150771 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 69125 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 69125 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 152365 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 152365 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 155941 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 155941 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 69126 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 69126 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 109174 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 109174 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 152548 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 152548 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 174219 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 174219 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 178399 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 178399 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 75526 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 75526 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 78373 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 78373 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 78373 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 152548 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 152548 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 158365 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 158365 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 20391 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 20391 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 20391 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 20797 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 20797 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 20797 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 62426 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 62426 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 62426 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 62426 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 69117 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 69117 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 156410 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 156410 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 6904 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 6904 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 6904 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 13814 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 13814 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 25931 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 25931 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 75917 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 75917 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 110434 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 110434 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 188617 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 188617 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 25879 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 25879 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 26019 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 26019 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 26020 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 26020 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 110420 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 110420 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 18693 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 18693 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 18693 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 108061 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 108061 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 108139 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 108139 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 108170 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 108170 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 13367 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 13367 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 108061 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 108061 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 108139 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 108139 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 108170 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 108170 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 9748 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 9748 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 9748 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 13334 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 13334 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 13335 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 13335 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 13408 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 13408 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 9748 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 9748 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 9748 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 59427 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 59427 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 209455 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 209455 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 124561 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 124561 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 108695 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 108695 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 18886 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 18886 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 18886 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 18207 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 18207 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 18207 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 20792 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 20792 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 20792 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 124555 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 124555 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 179534 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 179534 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 194648 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 194648 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 7253 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 7253 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 7253 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 7253 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 18198 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 18198 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 18198 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 110425 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 110425 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 13815 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 13815 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 32603 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 32603 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 18204 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 18204 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 18204 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 19848 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 19848 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 19848 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 25880 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 25880 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 26037 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 26037 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 13792 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 13792 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 211644 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 211644 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 211644 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 211644 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 13434 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 13434 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 13841 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 13841 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 14043 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 14043 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 190579 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 190579 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 209497 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 209497 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 20395 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 20395 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 20395 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 20672 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 20672 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 20672 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 153001 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 153001 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 201083 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 127663 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 127663 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 127663 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 10409 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 10409 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 10409 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 10409 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 10409 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 116424 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 116424 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 18903 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 18903 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 18903 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 18903 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 20789 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 20789 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 20789 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 156523 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 156523 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 156532 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 156532 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 9310 43 None -22 56 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 9310 43 None -22 56 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 9310 43 None -22 56 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 9310 43 None -22 56 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 9310 43 None -22 56 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 10640 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 10640 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 10640 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 10640 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 10640 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 10640 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 18203 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 18203 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 18203 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 27105 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 27105 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 8438 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 8438 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 8438 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 8438 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 209434 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 209434 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 18231 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 18231 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 18231 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 210840 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 210840 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 10633 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 10633 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 10633 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 10633 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 10633 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 10633 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 124553 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 124553 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 69123 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 69123 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 20398 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 20398 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 20398 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 25965 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 25965 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 25979 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 25979 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 179204 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 179204 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 96199 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 96199 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 179204 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 179204 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 108257 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 108257 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 166956 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 166956 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 194476 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 194476 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 183459 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 183459 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 108257 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 108257 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 166956 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 166956 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 183459 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 183459 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 194476 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 194476 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 179321 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 179321 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 179321 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 179321 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 9947 58 None -21 31 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 9947 58 None -21 31 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 9947 58 None -21 31 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 9947 58 None -21 31 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 9947 58 None -21 31 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 107833 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 107833 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 18208 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 18208 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 18208 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 183659 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 183659 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 74201 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 74201 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 74201 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 25930 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 25930 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 75918 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 75918 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 157579 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 157579 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 158366 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 158366 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 59491 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 59491 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 59491 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 21902 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 21902 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 205492 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 205492 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 18909 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 18909 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 18909 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 18884 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 18884 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 18884 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 18899 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 18899 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 18899 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 18895 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 18895 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 18895 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 69121 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 69121 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 69907 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 69907 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 69907 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 7741 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 7741 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 7741 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 7741 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 7741 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 9751 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 9751 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 9751 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 9641 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 9641 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 9641 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 9641 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 9641 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 124560 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 124560 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 213526 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 213526 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 213526 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 46813 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 46813 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 7191 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 7191 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 7191 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 7191 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 7191 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 212292 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 212292 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 212292 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 193699 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 193699 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 193699 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 69915 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 69915 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 69915 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 124558 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 124558 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 18904 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 18904 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 18904 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 167029 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 167029 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 69909 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 69909 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 69909 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 136078 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 136078 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 154721 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 154721 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 25990 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 25990 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 13432 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 13432 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 77893 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 77893 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 156887 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 156887 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 19174 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 19174 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 19174 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 25895 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 25895 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 13959 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 13959 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 127658 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 127658 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 127658 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 154825 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 154825 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 62426 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 62426 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 62426 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 62426 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 7311 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 7311 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 7311 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 7311 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 7311 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 149487 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 149487 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 136080 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 136080 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 124554 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 124554 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 159281 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 159281 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 156626 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 156626 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 69124 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 69124 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 75531 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 75531 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 75920 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 75920 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 110438 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 110438 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 110446 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 110446 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 110490 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 110490 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 110508 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 110508 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 6904 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 6904 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 6904 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 20798 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 20798 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 20798 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 9753 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 9753 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 9753 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 9753 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 9753 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 136080 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 136080 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 9957 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 9957 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 9957 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 9957 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 9957 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 108430 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 108430 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 108643 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 108643 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 20682 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 20682 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 20682 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 108430 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 108430 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 108643 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 108643 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 107864 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 107864 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 193678 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 193678 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 195174 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 195174 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 107864 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 107864 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 193678 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 193678 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 195174 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 195174 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 21974 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 21974 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 18907 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 18907 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 18907 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 7706 68 None -18 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 7706 68 None -18 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 7706 68 None -18 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 7706 68 None -18 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 7706 68 None -18 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
3500 8308 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 8308 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 8308 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 214458 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 214458 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 20088 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 20088 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 20088 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 157596 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 157596 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 69119 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 69119 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 18961 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 18961 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 18961 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 29425 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 29425 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 8963 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 8963 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 8963 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 8963 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 8963 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 20784 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 20784 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 20784 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 18213 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 18213 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 18213 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 8215 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 8215 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 8215 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 8215 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 8215 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 18190 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 18190 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 18190 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 110501 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 110501 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 26099 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 26099 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 75926 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 75926 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 13504 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 13504 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 13585 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 13585 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 21276 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 21276 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 18200 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 18200 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 18200 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 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
1213 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
2725 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
33036 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
4411 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
616 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
6976 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
716121 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
180 7189 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 7189 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 7189 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 7189 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 7189 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 85186 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 85186 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 85186 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 10633 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 10633 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 10633 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 10633 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 10633 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 10633 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 209575 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 209575 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 109127 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 109127 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 32917 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 32917 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 18206 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 18206 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 18206 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 209577 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 209577 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 109278 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 109278 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 18893 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 18893 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 18893 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 10519 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 10519 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 10519 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 10519 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 10519 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 10519 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 18868 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 18868 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 18868 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 67002 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 67002 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 151026 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 151026 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 75461 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 75461 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 75534 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 75534 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 75541 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 75541 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 75911 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 75911 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 75924 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 75924 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 110495 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 110495 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 110511 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 110511 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 110514 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 110514 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 7311 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 7311 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 7311 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 7311 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 7311 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 69112 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 69112 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 151692 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 151692 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 151268 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 151268 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 20564 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 20564 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 20564 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 25980 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 25980 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 107901 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 107901 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 200460 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 68228 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 68228 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 9905 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 9905 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 9905 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 9905 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 9905 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 126210 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 126210 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 107901 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 107901 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 108055 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 108055 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 194936 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 194936 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 108055 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 108055 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 209489 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 209489 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 152203 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 152203 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 160936 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 160936 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 167014 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 167014 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 26120 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 26120 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 110436 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 110436 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 194109 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 194109 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 211670 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 211670 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 211670 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 91160 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 91160 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 91160 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 213701 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 213701 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 213701 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 26061 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 26061 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 13480 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 13480 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 18908 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 18908 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 18908 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 7186 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 7186 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 7186 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 7186 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 7186 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 206508 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 206508 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 127659 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 127659 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 127659 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 174213 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 174213 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 174213 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 174213 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 8706 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 8706 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 8706 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 207401 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 207401 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 109665 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 109665 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 109665 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 22348 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 22348 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 22348 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 18214 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 18214 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 18214 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 85224 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 85224 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 18960 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 18960 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 18960 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 8439 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 8439 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 8439 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 8439 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 8439 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 136079 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 136079 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 124559 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 124559 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 207656 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 207656 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 35002 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 35002 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 18620 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 18620 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 18620 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 18620 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 7736 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 7736 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 7736 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 7736 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 7736 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 110509 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 110509 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 110510 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 110510 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 13584 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 13584 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 9688 112 None -27 65 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 9688 112 None -27 65 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 9688 112 None -27 65 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 9688 112 None -27 65 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
52943921 25896 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 25896 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 25913 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 25913 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 26005 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 26005 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 13433 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 13433 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 13945 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 13945 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 120493 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 120493 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 69116 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 69116 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 8196 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 8196 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 8196 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 8196 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 8196 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 159631 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 159631 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 18901 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 18901 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 18901 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 108295 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 108295 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 108460 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 108460 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 174898 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 174898 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 194757 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 194757 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 108295 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 108295 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 108460 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 108460 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 174898 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 174898 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 194757 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 194757 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 19931 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 19931 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 19931 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 18929 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 18929 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 18929 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 9956 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 9956 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 9956 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 9956 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 9956 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 201083 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 182928 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 182928 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 182928 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 182928 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 8171 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 8171 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 8171 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 8171 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 8171 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 21188 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 21188 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 18887 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 18887 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 18887 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 200460 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 90314 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 90314 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 18696 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 18696 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 18696 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 24758 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 24758 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 24758 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 195894 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 195894 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 18903 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 18903 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 18903 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 18903 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 8083 62 None -11 50 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 8083 62 None -11 50 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 8083 62 None -11 50 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 8083 62 None -11 50 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 8083 62 None -11 50 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 205863 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 205863 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 195694 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 195694 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 8443 50 None -407 65 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 8443 50 None -407 65 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 8443 50 None -407 65 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 8443 50 None -407 65 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 8443 50 None -407 65 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
4011 89183 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 89183 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 158580 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 158580 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 25991 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 25991 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 75545 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 75545 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 75921 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 75921 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 75922 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 75922 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 75927 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 75927 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 6904 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 6904 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 6904 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 20396 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 20396 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 20396 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 157367 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 157367 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 69120 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 69120 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 153806 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 153806 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 26121 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 26121 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 13189 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 13189 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 18202 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 18202 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 18202 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 18903 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 18903 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 18903 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 18903 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 18217 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 18217 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 18217 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 18217 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 18217 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 18217 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 18201 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 18201 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 18201 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 18866 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 18866 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 18866 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 125270 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 125270 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 108707 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 108707 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 18194 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 18194 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 18194 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 18194 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 18194 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 18194 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 97458 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 97458 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 7253 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 7253 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 7253 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 7253 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 195528 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 195528 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 127661 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 127661 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 127661 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 69910 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 69910 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 69910 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 20773 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 20773 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 20773 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 75525 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 75525 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 110496 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 110496 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 156733 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 156733 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 160184 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 160184 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 20800 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 20800 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 20800 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 10229 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 10229 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 10229 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 10229 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 10229 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 127660 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 127660 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 127660 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 9905 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 9905 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 9905 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 9905 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 9905 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 108051 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 108051 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 108051 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 108051 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 9748 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 9748 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 9748 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 184241 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 184241 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 9748 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 9748 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 9748 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 184241 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 184241 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 215379 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 18227 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 18227 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 18227 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 195785 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 195785 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 25859 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 25859 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 25860 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 25860 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 195018 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 195018 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 18903 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 18903 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 18903 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 18903 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 127655 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 127655 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 127655 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 21240 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 21240 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 21240 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 8214 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 8214 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 8214 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 8214 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 8214 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 8214 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 109635 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 109635 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 69118 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 69118 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 9370 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 9370 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 9370 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 9370 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 9370 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 18896 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 18896 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 18896 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 18189 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 18189 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 18189 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 18197 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 18197 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 18197 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 18199 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 18199 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 18199 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 63041 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 63041 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 20791 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 20791 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 20791 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 25950 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 25950 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 75928 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 75928 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 110423 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 110423 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 183802 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 183802 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 183802 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 183802 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 69115 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 69115 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 124557 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 124557 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 69122 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 69122 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 8063 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 8063 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 8063 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 8063 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 8063 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 20159 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 20159 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 20159 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 62032 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 62032 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 62032 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 11437 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 11437 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 114235 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 114235 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 7727 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 7727 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 7727 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 7727 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 7727 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 7745 93 None -10 90 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 7745 93 None -10 90 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 7745 93 None -10 90 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 7745 93 None -10 90 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 7745 93 None -10 90 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 26098 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 26098 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 69111 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 69111 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 158005 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 158005 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 159535 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 159535 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 154578 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 154578 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 11524 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 11524 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 97459 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 97459 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 7293 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 7293 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 7293 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 7293 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 7293 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 18209 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 18209 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 18209 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 18193 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 18193 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 18193 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 79068 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 79068 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 18221 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 18221 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 18221 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 18195 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 18195 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 18195 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 18195 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 18195 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 18195 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 7581 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 7581 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 7581 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 7581 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 7581 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 18883 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 18883 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 18883 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 124557 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 124557 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 154481 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 154481 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 10577 58 None -8 54 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 10577 58 None -8 54 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 10577 58 None -8 54 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 10577 58 None -8 54 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 10577 58 None -8 54 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 7581 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 7581 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 7581 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 7581 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 7581 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 18187 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 18187 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 18187 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 202093 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 202093 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 9793 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 9793 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 9793 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 9905 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 9905 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 9905 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 9905 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 9905 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 56579 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 56579 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 121564 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 121564 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 11551 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 11551 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 192156 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 192156 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 199747 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 199747 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 199747 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 199798 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 199798 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 199798 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 199810 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 199810 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 199810 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 12706 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 12706 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 12706 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 7311 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 7311 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 7311 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 7311 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 7311 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 19530 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 19530 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 20440 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 20440 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 20440 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 88933 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 88933 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 88933 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 88934 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 88934 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 20508 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 20508 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 20508 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 18057 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 18057 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 18057 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 17919 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 17919 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 17919 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 201083 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 201083 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 20499 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 20499 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 20499 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 20261 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 20261 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 20261 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 20478 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 20478 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 20478 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 200460 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 20280 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 20280 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 20280 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 200460 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 148693 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 148693 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 65312 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 65312 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 119600 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 119600 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 119600 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 199381 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 199381 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 119597 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 119597 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 119597 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 139793 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 139793 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 113232 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 113232 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 113232 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 125830 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 125830 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 119563 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 119563 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 119563 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 85161 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 85161 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 85161 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 10711 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 10711 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 10711 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 10711 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 10711 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 10711 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 113231 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 113231 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 113231 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 221098 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 7698 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 7698 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 7698 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 198042 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 198042 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 85161 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 85161 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 85161 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 119592 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 119592 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 119592 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 184071 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 184071 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 184071 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 184071 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 20683 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 20683 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 20683 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 185033 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 185033 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 185033 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 185041 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 185041 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 185041 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 198285 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 198285 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 125824 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 125824 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 79673 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 79673 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 20798 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 20798 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 20798 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 200878 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 184371 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 184371 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 68568 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 68568 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 115400 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 115400 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 221025 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 221233 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 192865 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 192865 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 119599 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 119599 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 119599 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 125834 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 125834 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 125841 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 125841 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 131177 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 131177 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 131979 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 131979 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 131980 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 131980 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 131981 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 131981 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 131982 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 131982 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 131983 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 131983 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 131984 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 131984 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 131985 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 131985 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 131986 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 131986 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 131987 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 131987 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 131988 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 131988 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 131989 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 131989 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 131990 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 131990 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 131991 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 131991 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 131992 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 131992 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 131993 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 131993 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 131994 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 131994 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 131995 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 131995 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 131996 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 131996 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 131998 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 131998 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 132000 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 132000 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 132003 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 132003 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 132011 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 132011 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 132014 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 132014 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 132015 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 132015 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 132017 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 132017 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 132020 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 132020 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 132031 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 132031 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 132032 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 132032 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 132033 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 132033 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 132034 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 132034 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 132035 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 132035 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 132037 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 132037 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 132039 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 132039 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 132040 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 132040 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 132042 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 132042 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 132049 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 132049 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 132051 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 132051 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 132053 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 132053 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 132054 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 132054 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 132056 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 132056 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 132058 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 132058 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 132059 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 132059 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 132060 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 132060 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 132064 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 132064 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 132066 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 132066 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 132067 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 132067 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 132069 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 132069 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 132070 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 132070 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 132071 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 132071 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 132073 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 132073 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 135245 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 135245 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 150050 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 150050 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 158584 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 158584 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 167558 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 167558 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 131177 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 131177 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 131979 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 131979 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 131980 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 131980 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 131981 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 131981 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 131982 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 131982 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 131983 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 131983 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 131984 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 131984 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 131985 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 131985 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 131986 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 131986 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 131987 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 131987 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 131988 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 131988 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 131989 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 131989 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 131990 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 131990 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 131991 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 131991 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 131992 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 131992 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 131993 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 131993 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 131994 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 131994 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 131995 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 131995 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 131996 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 131996 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 131998 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 131998 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 132000 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 132000 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 132003 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 132003 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 132011 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 132011 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 132014 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 132014 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 132015 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 132015 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 132017 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 132017 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 132020 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 132020 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 132024 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 132024 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 132029 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 132029 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 132031 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 132031 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 132032 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 132032 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 132033 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 132033 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 132034 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 132034 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 132035 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 132035 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 132037 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 132037 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 132038 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 132038 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 132039 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 132039 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 132040 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 132040 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 132042 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 132042 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 132049 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 132049 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 132051 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 132051 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 132053 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 132053 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 132054 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 132054 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 132056 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 132056 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 132059 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 132059 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 132060 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 132060 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 132064 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 132064 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 132066 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 132066 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 132067 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 132067 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 132068 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 132068 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 132069 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 132069 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 132070 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 132070 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 132071 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 132071 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 132072 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 132072 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 132073 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 132073 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 131177 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 131177 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 131979 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 131979 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 131980 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 131980 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 131981 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 131981 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 131982 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 131982 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 131983 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 131983 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 131984 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 131984 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 131985 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 131985 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 131986 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 131986 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 131987 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 131987 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 131989 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 131989 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 131990 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 131990 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 131991 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 131991 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 131992 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 131992 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 131993 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 131993 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 131994 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 131994 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 131995 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 131995 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 131996 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 131996 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 131998 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 131998 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 132000 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 132000 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 132003 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 132003 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 132006 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 132006 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 132011 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 132011 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 132014 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 132014 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 132015 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 132015 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 132017 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 132017 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 132020 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 132020 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 132024 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 132024 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 132029 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 132029 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 132031 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 132031 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 132032 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 132032 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 132033 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 132033 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 132034 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 132034 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 132035 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 132035 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 132037 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 132037 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 132038 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 132038 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 132039 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 132039 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 132040 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 132040 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 132042 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 132042 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 132049 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 132049 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 132051 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 132051 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 132053 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 132053 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 132054 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 132054 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 132056 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 132056 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 132059 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 132059 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 132060 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 132060 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 132064 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 132064 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 132066 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 132066 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 132067 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 132067 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 132070 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 132070 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 132071 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 132071 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 132072 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 132072 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 132073 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 132073 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 135243 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 135243 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 135244 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 135244 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 135245 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 135245 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 74702 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 74702 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 7311 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 7311 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 7311 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 7311 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 7311 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 119240 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 119240 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 119602 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 119602 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 119602 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 221094 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 221098 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 222088 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 191318 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 191318 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 191752 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 191752 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 192883 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 192883 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 191752 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 191752 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 197627 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 197627 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 147477 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 147477 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 65312 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 65312 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 74710 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 74710 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 86316 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 86316 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 147477 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 147477 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 19534 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 19534 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 19534 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 201083 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 65313 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 65313 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 65314 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 65314 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 69910 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 69910 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 69910 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 200460 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 200460 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 200436 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 201083 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 221138 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 221227 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 221233 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 221265 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 191650 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 191650 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 199264 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 199264 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 110160 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 110160 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 125828 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 125828 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 202662 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 202662 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 211030 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 211030 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 81055 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 81055 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 81055 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 152592 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 152592 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 74719 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 74719 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 185101 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 185101 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 185101 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 145992 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 145992 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 65315 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 65315 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 62426 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 62426 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 62426 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 62426 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 74705 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 74705 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 136078 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 136078 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 136079 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 136079 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 119564 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 119564 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 119564 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 87337 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 87337 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 221203 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 221220 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 221227 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 221691 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 222043 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 198734 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 198734 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 173859 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 173859 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 125825 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 125825 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 125827 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 125827 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 125842 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 125842 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 79749 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 79749 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 119250 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 119250 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 131997 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 131997 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 131999 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 131999 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 132001 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 132001 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 132004 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 132004 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 132007 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 132007 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 132008 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 132008 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 132009 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 132009 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 132010 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 132010 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 132013 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 132013 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 132016 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 132016 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 132018 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 132018 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 132022 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 132022 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 132023 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 132023 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 132025 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 132025 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 132027 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 132027 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 132028 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 132028 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 132030 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 132030 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 132038 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 132038 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 132044 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 132044 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 132046 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 132046 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 132052 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 132052 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 132055 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 132055 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 132057 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 132057 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 132061 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 132061 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 132062 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 132062 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 132065 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 132065 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 132069 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 132069 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 160447 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 160447 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 131997 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 131997 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 131999 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 131999 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 132001 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 132001 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 132002 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 132002 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 132004 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 132004 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 132007 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 132007 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 132008 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 132008 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 132009 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 132009 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 132010 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 132010 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 132013 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 132013 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 132016 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 132016 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 132018 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 132018 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 132022 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 132022 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 132023 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 132023 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 132025 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 132025 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 132027 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 132027 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 132028 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 132028 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 132030 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 132030 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 132038 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 132038 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 132044 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 132044 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 132046 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 132046 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 132052 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 132052 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 132055 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 132055 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 132057 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 132057 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 132058 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 132058 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 132061 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 132061 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 132062 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 132062 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 132065 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 132065 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 132069 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 132069 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 131997 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 131997 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 131999 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 131999 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 132001 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 132001 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 132002 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 132002 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 132004 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 132004 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 132007 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 132007 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 132008 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 132008 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 132009 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 132009 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 132010 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 132010 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 132013 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 132013 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 132016 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 132016 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 132018 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 132018 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 132022 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 132022 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 132023 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 132023 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 132025 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 132025 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 132027 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 132027 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 132028 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 132028 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 132030 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 132030 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 132038 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 132038 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 132044 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 132044 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 132046 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 132046 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 132052 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 132052 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 132055 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 132055 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 132057 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 132057 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 132058 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 132058 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 132061 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 132061 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 132062 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 132062 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 132065 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 132065 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 132069 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 132069 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 74704 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 74704 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 119552 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 119552 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 119552 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 62426 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 62426 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 62426 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 62426 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 94799 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 94799 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 6904 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 6904 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 6904 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 136080 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 136080 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 185081 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 185081 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 185081 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 21255 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 21255 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 21255 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 85693 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 85693 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 79602 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 79602 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 79684 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 79684 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 119595 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 119595 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 119595 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 184954 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 184954 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 221805 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 222026 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 191228 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 191228 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 192571 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 192571 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 100035 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 100035 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 85685 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 85685 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 100035 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 100035 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 7384 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 7384 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 7384 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 7384 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 7384 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 7384 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 68569 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 68569 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 201018 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 62426 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 62426 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 62426 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 62426 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 130769 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 130769 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 87550 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 87550 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 87550 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 87550 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 132019 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 132019 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 132036 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 132036 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 132041 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 132041 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 132045 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 132045 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 132048 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 132048 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 132050 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 132050 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 157032 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 157032 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 132012 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 132012 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 132019 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 132019 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 132036 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 132036 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 132041 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 132041 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 132045 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 132045 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 132048 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 132048 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 132050 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 132050 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 132012 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 132012 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 132019 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 132019 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 132036 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 132036 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 132041 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 132041 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 132045 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 132045 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 132048 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 132048 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 132050 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 132050 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 68592 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 68592 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 85691 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 85691 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 68592 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 68592 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 113235 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 113235 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 113235 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 221237 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 221549 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 221716 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 221763 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 221827 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 221954 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 192360 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 192360 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 199203 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 199203 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 62426 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 62426 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 62426 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 62426 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 103544 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 103544 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 165319 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 165319 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 125833 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 125833 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 125835 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 125835 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 125840 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 125840 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 87550 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 87550 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 173062 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 173062 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 65311 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 65311 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 200236 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 18618 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 18618 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 18618 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 130763 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 130763 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 184717 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 184717 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 184331 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 184331 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 184658 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 184658 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 119594 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 119594 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 119594 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 86431 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 86431 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 116109 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 116109 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 184893 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 184893 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 146013 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 146013 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 175722 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 175722 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 68570 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 68570 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 221224 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 221227 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 221887 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 191775 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 191775 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 193105 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 193105 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 79650 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 79650 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 6904 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 6904 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 6904 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 183360 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 183360 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 183360 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 132021 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 132021 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 132043 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 132043 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 132021 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 132021 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 132043 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 132043 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 132021 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 132021 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 132043 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 132043 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 6904 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 6904 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 6904 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 7311 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 7311 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 7311 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 7311 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 7311 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 6904 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 6904 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 6904 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 183453 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 183453 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 183453 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 113302 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 113302 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 113302 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 85694 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 85694 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 184658 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 184658 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 184055 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 184055 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 115400 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 115400 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 211037 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 211037 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 211037 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 211037 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 87067 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 87067 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 7311 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 7311 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 7311 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 7311 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 7311 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 221246 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 221307 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 221732 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 125832 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 125832 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 183411 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 183411 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 183411 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 86735 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 86735 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 87131 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 87131 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 86311 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 86311 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 65303 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 65303 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 184603 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 184603 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 7311 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 7311 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 7311 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 7311 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 7311 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 87566 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 87566 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 86427 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 86427 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 109376 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 109376 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 109376 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 9753 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 9753 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 9753 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 9753 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 9753 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 19069 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 19069 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 19069 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 201254 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 79679 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 79679 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 184675 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 184675 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 221277 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 221833 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 222250 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 125829 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 125829 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 125836 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 125836 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 125841 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 125841 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 68589 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 68589 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 184304 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 184304 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 183267 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 183267 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 183267 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 18622 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 18622 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 18622 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 6904 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 6904 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 6904 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 143740 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 143740 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 116119 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 116119 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 130762 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 130762 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 65310 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 65310 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 19068 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 19068 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 19068 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 65305 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 65305 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 91677 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 91677 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 85695 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 85695 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 68555 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 68555 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 200795 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 9753 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 9753 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 9753 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 9753 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 9753 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 147689 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 147689 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 148093 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 148093 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 62426 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 62426 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 62426 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 62426 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 221358 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 221800 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 197641 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 197641 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 198715 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 198715 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 122553 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 122553 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 125839 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 125839 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 212912 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 212912 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 7311 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 7311 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 7311 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 7311 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 7311 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 132063 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 132063 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 132063 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 132063 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 132063 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 132063 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 17319 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 17319 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 65312 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 65312 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 62426 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 62426 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 62426 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 62426 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 189531 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 189531 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 185065 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 185065 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 185065 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 183206 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 183206 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 183206 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 183393 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 183393 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 183393 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 183420 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 183420 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 183420 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 148421 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 148421 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 185098 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 185098 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 185098 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 7311 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 7311 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 7311 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 7311 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 7311 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 184354 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 184354 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 18621 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 18621 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 18621 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 86993 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 86993 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 8196 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 8196 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 8196 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 8196 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 8196 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 119554 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 119554 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 119554 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 9753 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 9753 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 9753 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 9753 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 9753 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 183995 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 183995 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 91421 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 91421 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 100035 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 100035 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 109906 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 109906 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 68591 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 68591 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 85692 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 85692 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 79800 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 79800 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 81768 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 81768 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 147574 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 147574 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 197167 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 197167 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 200439 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 184899 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 184899 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 125843 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 125843 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 212900 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 212900 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 74176 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 74176 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 74176 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 148788 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 148788 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 122554 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 122554 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 210785 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 210785 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 116123 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 116123 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 116125 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 116125 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 41699 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 41699 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 130764 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 130764 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 184592 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 184592 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 183268 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 183268 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 183268 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 114323 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 114323 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 6904 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 6904 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 6904 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 6904 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 6904 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 6904 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 210592 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 210592 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 201083 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 146009 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 146009 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 221462 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 221512 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 192702 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 192702 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 125831 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 125831 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 212798 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 212798 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 9753 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 9753 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 9753 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 9753 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 9753 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 80681 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 80681 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 116131 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 116131 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 94729 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 94729 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 211092 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 211092 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 90217 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 90217 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 68588 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 68588 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 83960 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 83960 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 83960 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 155639 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 155639 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 184685 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 184685 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 183172 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 183172 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 183172 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 136080 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 136080 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 9753 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 9753 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 9753 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 9753 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 9753 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 83953 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 83953 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 83953 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 20810 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 20810 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 20810 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 83953 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 83953 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 83953 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 113233 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 113233 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 113233 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 198367 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 198367 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 125826 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 125826 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 113713 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 113713 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 65306 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 65306 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 88092 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 88092 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 91439 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 91439 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 204460 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 204460 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 144656 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 144656 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 106671 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 106671 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 210307 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 210307 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 185045 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 185045 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 185045 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 183208 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 183208 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 183208 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 144300 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 144300 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 91538 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 91538 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 18006 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 18006 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 18006 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 65304 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 65304 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 119593 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 119593 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 119593 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 74700 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 74700 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 201158 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 100808 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 100808 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 143749 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 143749 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 91474 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 91474 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 143985 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 143985 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 74699 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 74699 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 144623 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 144623 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 183130 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 183130 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 183130 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 184957 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 184957 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 113234 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 113234 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 113234 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 110167 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 110167 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 103517 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 103517 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 109174 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 109174 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 125845 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 125845 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 111144 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 111144 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 212497 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 212497 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 10409 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 10409 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 10409 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 10409 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 10409 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 79619 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 79619 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 221246 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 221549 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 221805 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 116114 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 116114 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 193359 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 193359 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 107924 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 107924 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 107924 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 107924 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 107924 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 107924 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 199176 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 199176 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 72762 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 72762 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 167667 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 167667 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 122555 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 122555 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 83930 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 83930 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 84099 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 84099 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 171011 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 171011 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 104433 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 104433 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 104433 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 104433 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 18800 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 18800 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 18800 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 115400 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 115400 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 211160 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 211160 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 7745 93 None -10 90 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 7745 93 None -10 90 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 7745 93 None -10 90 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 7745 93 None -10 90 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 7745 93 None -10 90 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 9688 112 None -27 65 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 9688 112 None -27 65 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 9688 112 None -27 65 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 9688 112 None -27 65 Human 7.0 pKi = 7 Binding
Binding affinity to M3 receptor (unknown origin) by PDSP assayBinding affinity to M3 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
44406387 79618 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 79618 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 79717 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 79717 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 7239 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 7239 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 7239 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 89183 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 89183 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 183359 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 183359 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 183359 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 83545 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 83545 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 147220 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 147220 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 173132 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 173132 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 111121 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 111121 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 104905 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 104905 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 47313 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 47313 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 11702 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 11702 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 79445 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 79445 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 144778 0 None -39 4 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 144778 0 None -39 4 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 195694 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 195694 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 212853 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 212853 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 105869 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 105869 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 183086 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 183086 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 183086 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 164584 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 164584 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 72469 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 72469 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 8443 50 None -407 65 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 8443 50 None -407 65 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 8443 50 None -407 65 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 8443 50 None -407 65 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 8443 50 None -407 65 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
16125444 175206 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 175206 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 75941 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 75941 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 181929 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 181929 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 12046 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 12046 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 8706 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 8706 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 8706 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 168159 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 168159 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 7581 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 7581 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 7581 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 7581 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 7581 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 127079 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 127079 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 195312 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 195312 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 195312 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 20895 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 20895 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 20895 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 91535 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 91535 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 99309 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 99309 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 187254 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 187254 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 210275 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 210275 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 96573 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 96573 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 183359 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 183359 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 183359 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 162533 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 162533 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 162533 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 24450 0 None -1479 12 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 24450 0 None -1479 12 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 9281 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 9281 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 9281 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 9281 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 185090 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 185090 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 185090 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 9281 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 9281 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 9281 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 9281 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 9281 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 9281 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 9281 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 9281 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 174584 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 174584 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 188051 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 188051 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 20912 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 20912 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 20912 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 210293 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 210293 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 175287 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 175287 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 184003 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 184003 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 45057 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 45057 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 126040 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 126040 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 16037 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 16037 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 96577 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 96577 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 167773 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 167773 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 167773 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 8215 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 8215 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 8215 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 8215 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 8215 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 117343 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 117343 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 91107 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 91107 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 143528 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 143528 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 28465 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 28465 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 28465 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 111503 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 111503 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 195265 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 195265 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 195265 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 183290 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 183290 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 183290 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 187741 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 187741 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 183614 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 183614 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 176835 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 176835 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 108938 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 108938 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 91553 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 91553 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 64603 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 64603 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 65869 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 65869 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 122557 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 122557 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 76101 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 76101 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 119555 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 119555 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 119555 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 200317 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 47101 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 47101 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 101158 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 101158 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 161563 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 161563 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 116450 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 116450 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 221224 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 211174 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 211174 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 109375 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 109375 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 101397 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 101397 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 167828 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 167828 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 167828 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 167895 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 167895 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 167895 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 86425 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 86425 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 195320 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 195320 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 195320 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 122550 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 122550 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 188597 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 188597 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 183616 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 183616 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 211278 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 211278 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 90576 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 90576 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 19108 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 19108 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 19108 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 19747 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 19747 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 19747 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 195528 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 195528 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 183290 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 183290 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 183290 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 183376 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 183376 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 183376 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 82829 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 82829 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 146019 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 146019 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 7581 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 7581 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 7581 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 7581 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 7581 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 190523 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 190523 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 190523 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 179692 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 179692 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 215379 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 186218 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 186218 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 142036 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 142036 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 10869 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 10869 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 10869 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 10869 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 10869 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 150429 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 150429 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 82702 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 82702 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 46107 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 46107 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 177729 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 177729 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 10409 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 10409 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 10409 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 10409 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 10409 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 175678 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 175678 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 176121 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 176121 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 183372 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 183372 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 183372 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 211113 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 211113 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 148310 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 148310 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 180740 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 180740 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 195018 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 195018 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 208581 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 208581 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 212701 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 212701 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 167947 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 167947 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 167947 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 99320 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 99320 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 85357 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 85357 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 195246 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 195246 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 195246 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 185107 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 185107 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 185107 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 185108 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 185108 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 185108 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 180687 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 180687 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 195785 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 195785 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 185016 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 185016 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 185016 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 164362 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 164362 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 11848 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 11848 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 11848 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 21240 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 21240 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 21240 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 8214 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 8214 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 8214 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 8214 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 8214 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 8214 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 109635 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 109635 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 18217 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 18217 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 18217 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 10339 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 10339 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 10339 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 183333 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 183333 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 183333 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 11679 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 11679 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 7581 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 7581 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 7581 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 7581 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 7581 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 63629 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 63629 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 63629 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 63629 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 75444 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 75444 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 155804 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 155804 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 65290 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 65290 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 200460 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 183824 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 183824 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 126361 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 126361 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 136078 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 136078 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 185021 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 185021 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 185021 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 65318 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 65318 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 167789 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 167789 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 167789 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 178901 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 178901 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 93728 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 93728 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 167772 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 167772 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 167772 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 9370 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 9370 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 9370 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 9370 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 9370 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 117343 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 117343 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 83842 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 83842 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 163845 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 163845 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 185030 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 185030 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 185030 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 168370 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 168370 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 18651 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 18651 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 18651 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 185084 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 185084 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 185084 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 10636 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 10636 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 10636 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 185084 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 185084 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 185084 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 10636 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 10636 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 10636 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 183205 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 183205 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 183205 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 208638 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 208638 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 63041 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 63041 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 47406 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 47406 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 167819 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 167819 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 167819 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 167819 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 93781 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 93781 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 166160 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 166160 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 212605 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 212605 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 208590 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 208590 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 19073 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 19073 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 19073 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 109742 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 214561 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 214561 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 107759 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 107759 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 107759 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 107759 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 107759 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 107759 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 117966 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 117966 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 183113 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 183113 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 183113 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 117966 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 117966 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 105545 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 105545 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 199476 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 199476 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 91123 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 91123 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 91479 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 91479 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 183388 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 183388 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 183388 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 185026 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 185026 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 185026 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 20806 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 20806 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 20806 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 104103 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 104103 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 104103 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 104103 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 130669 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 130669 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 65833 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 65833 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 185037 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 185037 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 185037 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 168310 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 168310 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 12003 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 12003 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 177473 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 177473 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 9905 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 9905 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 9905 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 9905 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 9905 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 99081 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 99081 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 82303 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 82303 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 7239 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 7239 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 7239 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 158868 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 158868 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 212541 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 212541 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 212859 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 212859 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 122267 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 122267 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 183334 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 183334 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 183334 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 148693 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 148693 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 8063 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 8063 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 8063 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 8063 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 8063 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 210746 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 210746 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 62032 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 62032 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 62032 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 93781 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 93781 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 82809 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 82809 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 84087 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 84087 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 45165 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 45165 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 183204 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 183204 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 183204 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 104105 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 104105 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 91960 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 91960 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 185094 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 185094 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 185094 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 106650 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 106650 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 78977 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 78977 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 145160 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 145160 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 167749 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 167749 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 167749 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 90578 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 90578 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 90578 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 90578 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 7727 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 7727 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 7727 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 7727 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 7727 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 194632 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 194632 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 194632 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 108787 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 108787 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 183066 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 183066 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 183066 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 168332 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 168332 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 20897 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 20897 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 20897 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 91554 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 91554 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 105746 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 105746 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 204268 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 204268 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 86885 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 86885 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 185024 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 185024 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 185024 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 185097 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 185097 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 185097 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 168411 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 168411 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 109787 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 109787 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 172428 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 172428 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 7745 93 None -10 90 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 7745 93 None -10 90 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 7745 93 None -10 90 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 7745 93 None -10 90 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 7745 93 None -10 90 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 65289 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 65289 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 183171 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 183171 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 183171 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 46492 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 46492 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 49050 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 49050 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 198430 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 198430 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 18597 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 18597 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 18597 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 118253 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 118253 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 90568 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 90568 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 90577 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 90577 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 90577 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 90577 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 195386 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 195386 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 195386 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 176143 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 176143 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 89053 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 89053 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 187935 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 187935 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 18681 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 18681 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 18681 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 127555 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 127555 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 83954 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 83954 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 83954 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 164817 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 164817 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 176586 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 176586 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 176586 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 99576 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 99576 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 7293 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 7293 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 7293 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 7293 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 7293 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 99310 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 99310 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 140381 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 140381 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 94758 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 94758 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 116112 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 116112 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 130766 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 130766 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 45176 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 45176 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 128763 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 128763 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 194239 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 194239 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 144114 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 144114 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 210085 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 210085 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 210085 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 210085 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 127598 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 127598 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 195520 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 195520 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 183087 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 183087 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 183087 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 85176 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 85176 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 184637 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 184637 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 86310 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 86310 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 10577 58 None -8 54 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 10577 58 None -8 54 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 10577 58 None -8 54 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 10577 58 None -8 54 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 10577 58 None -8 54 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 94092 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 94092 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 65302 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 65302 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 185110 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 185110 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 185110 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 182226 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 182226 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 183207 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 183207 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 183207 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 126035 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 126035 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 168302 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 168302 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 128758 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 128758 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 91021 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 91021 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 126786 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 126786 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 126786 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 127565 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 127565 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 122558 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 122558 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 194238 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 194238 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 202487 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 202487 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 201471 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 201471 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 210658 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 210658 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 16167 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 16167 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 197366 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 197366 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 122560 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 122560 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 194715 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 194715 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 167751 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 167751 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 167751 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 167751 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 90097 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 90097 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 144664 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 144664 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 10159 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 10159 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 10159 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 185117 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 185117 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 185117 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 16102 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 16102 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 16102 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 16102 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 45460 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 45460 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 77244 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 77244 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 116121 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 116121 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 116126 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 116126 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 138216 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 138216 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 94761 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 94761 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 136080 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 136080 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 42189 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 42189 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 42189 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 200460 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 7311 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 7311 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 7311 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 7311 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 7311 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 144933 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 144933 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 83956 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 83956 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 83956 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 201083 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 85697 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 85697 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 116110 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 116110 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 72764 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 72764 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 183830 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 183830 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 183385 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 183385 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 183385 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 201083 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 128468 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 128468 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 91422 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 91422 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 200460 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 86610 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 86610 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 143995 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 143995 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 79497 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 79497 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 94796 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 94796 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 65307 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 65307 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 72763 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 72763 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 6904 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 6904 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 6904 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 45320 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 45320 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 221220 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 110179 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 110179 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 113259 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 113259 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 113259 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 102615 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 102615 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 102880 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 102880 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 212686 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 212686 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 91565 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 91565 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 65308 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 65308 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 200946 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 179829 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 179829 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 183466 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 183466 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 183466 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 9266 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 9266 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 9266 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 9266 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 9266 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 91331 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 91331 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 94797 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 94797 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 91507 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 91507 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 185096 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 185096 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 185096 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 144924 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 144924 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 210790 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 210790 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 91429 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 91429 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 183105 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 183105 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 183105 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 86572 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 86572 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 210790 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 210790 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 41929 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 41929 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 109610 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 109610 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 152929 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 152929 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 18830 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 18830 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 18830 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 147302 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 147302 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 94757 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 94757 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 94759 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 94759 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 94002 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 94002 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 100889 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 100889 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 178189 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 178189 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 183140 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 183140 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 183140 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 86430 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 86430 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 99082 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 99082 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 158868 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 158868 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 147352 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 147352 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 167771 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 167771 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 167771 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 184032 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 184032 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 214146 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 214146 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 7581 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 7581 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 7581 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 7581 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 7581 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 167783 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 167783 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 167783 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 202356 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 202356 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 202356 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 11731 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 11731 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 91540 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 91540 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 91710 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 91710 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 194659 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 194659 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 194659 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 9748 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 9748 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 9748 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 105530 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 105530 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 204942 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 204942 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 127036 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 127036 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 90572 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 90572 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 90572 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 90572 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 78806 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 78806 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 208583 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 208583 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 45125 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 45125 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 185100 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 185100 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 185100 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 167920 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 167920 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 167920 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 167816 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 167816 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 167816 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 11551 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 11551 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 18035 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 18035 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 18035 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 99317 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 99317 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 98952 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 98952 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 63320 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 63320 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 87383 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 87383 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 83957 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 83957 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 83957 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 16550 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 16550 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 16550 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 20906 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 20906 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 20906 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 99316 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 99316 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 24526 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 24526 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 24526 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 24526 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 11993 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 11993 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 91539 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 91539 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 187850 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 187850 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 116115 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 116115 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 65286 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 65286 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 91510 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 91510 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 182264 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 182264 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 47295 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 47295 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 127036 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 127036 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 185062 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 185062 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 185062 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 90573 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 90573 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 172958 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 172958 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 11794 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 11794 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 105807 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 105807 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 196198 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 196198 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 94091 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 94091 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 19087 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 19087 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 19087 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 20866 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 20866 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 20866 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 204488 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 204488 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 194715 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 194715 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 179534 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 179534 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 130788 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 130788 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 165988 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 165988 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 185015 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 185015 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 185015 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 18624 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 18624 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 18624 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 168815 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 168815 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 19076 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 19076 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 19076 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 9251 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 9251 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 9251 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 9251 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 9251 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 9251 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 9251 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 9251 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 9251 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 9251 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 9251 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 9251 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 9251 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 9251 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 9251 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 185040 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 185040 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 185040 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 165015 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 165015 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 127088 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 127088 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 18686 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 18686 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 18686 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 18686 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 18686 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 9905 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 9905 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 9905 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 9905 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 9905 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 210446 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 210446 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 210826 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 210826 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 167748 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 167748 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 167748 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 20038 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 20038 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 173039 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 173039 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 151454 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 151454 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 75443 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 75443 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 78977 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 78977 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 65295 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 65295 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 83521 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 83521 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 147360 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 147360 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 100807 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 100807 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 88933 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 88933 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 88933 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 196746 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 196746 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 198286 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 198286 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 212916 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 212916 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 212951 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 212951 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 213112 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 213112 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 213233 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 213233 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 88933 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 88933 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 88933 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 172190 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 172190 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 175456 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 175456 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 177724 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 177724 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 176789 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 176789 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 167788 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 167788 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 167788 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 82324 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 82324 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 83528 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 83528 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 195294 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 195294 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 195294 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 90032 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 90032 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 7239 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 7239 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 7239 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 103324 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 103324 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 103324 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 127117 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 127117 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 103895 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 103895 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 103895 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 103895 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 88894 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 88894 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 88894 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 183615 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 183615 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 82474 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 82474 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 91917 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 91917 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 96588 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 96588 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 9793 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 9793 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 9793 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 187541 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 187541 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 7670 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 7670 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 7670 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 7670 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 7670 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 28546 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 28546 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 28546 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 189356 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 189356 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 12352 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 12352 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 211102 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 211102 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 78465 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 78465 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 116113 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 116113 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 136079 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 136079 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 91555 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 91555 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 194909 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 194909 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 194909 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 177466 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 177466 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 214359 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 214359 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 172589 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 172589 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 127151 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 127151 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 194575 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 194575 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 194575 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 12351 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 12351 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 168325 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 168325 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 188513 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 188513 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 211644 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 211644 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 211644 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 211644 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 168140 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 168140 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 210501 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 210501 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 183303 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 183303 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 183303 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 195807 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 195807 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 195807 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 127605 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 127605 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 127605 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 65285 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 65285 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 200722 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 183280 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 183280 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 183280 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 86315 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 86315 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 109378 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 109378 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 109378 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 180884 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 180884 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 126338 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 126338 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 178464 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 178464 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 93733 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 93733 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 18680 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 18680 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 18680 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 138883 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 138883 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 185902 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 185902 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 185902 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 11897 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 11897 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 87381 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 87381 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 182080 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 182080 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 9281 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 9281 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 9281 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 9281 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 86309 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 86309 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 9905 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 9905 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 9905 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 9905 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 9905 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 128277 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 128277 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 79170 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 79170 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 65309 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 65309 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 119589 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 119589 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 119589 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 178831 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 178831 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 183139 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 183139 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 183139 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 7030 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 7030 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 7030 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 180745 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 180745 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 45931 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 45931 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 109447 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 109447 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 127289 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 127289 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 199993 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 199993 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 11803 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 11803 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 91131 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 91131 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 92977 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 92977 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 65997 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 65997 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 194908 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 194908 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 194908 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 186913 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 186913 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 189654 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 189654 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 183679 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 183679 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 18600 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 18600 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 18600 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 85205 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 85205 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 109871 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 109871 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 177752 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 177752 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 77773 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 77773 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 107241 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 107241 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 107241 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 187600 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 187600 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 9310 43 None -22 56 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 9310 43 None -22 56 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 9310 43 None -22 56 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 9310 43 None -22 56 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 9310 43 None -22 56 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 86234 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 86234 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 91438 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 91438 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 28488 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 28488 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 116134 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 116134 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 200346 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 46531 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 46531 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 96587 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 96587 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 91533 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 91533 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 10633 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 10633 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 10633 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 10633 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 10633 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 10633 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 82803 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 82803 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 221267 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 197216 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 197216 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 197288 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 197288 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 113252 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 113252 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 113252 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 82803 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 82803 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 125838 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 125838 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 10614 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 10614 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 10614 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 10614 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 10614 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 141151 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 141151 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 201251 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 82803 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 82803 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 82803 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 82803 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 127788 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 127788 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 68240 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 68240 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 108967 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 108967 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 155800 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 155800 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 170251 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 170251 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 208582 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 208582 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 48746 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 48746 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 127765 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 127765 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 140381 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 140381 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 128188 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 128188 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 83963 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 83963 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 83963 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 110330 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 110330 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 166899 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 166899 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 116111 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 116111 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 130765 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 130765 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 130768 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 130768 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 146015 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 146015 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 183403 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 183403 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 183403 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 46561 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 46561 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 74703 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 74703 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 191992 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 191992 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 193338 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 193338 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 197864 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 197864 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 198330 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 198330 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 141151 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 141151 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 212542 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 212542 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 212838 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 212838 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 10640 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 10640 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 10640 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 10640 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 10640 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 10640 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 18683 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 18683 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 18683 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 18683 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 184801 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 184801 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 46596 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 46596 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 184933 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 184933 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 182012 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 182012 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 112949 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 112949 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 9452 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 9452 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 9452 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 163740 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 163740 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 194210 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 194210 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 64183 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 64183 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 27105 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 27105 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 127414 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 127414 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 11730 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 11730 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 106587 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 106587 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 100845 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 100845 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 175174 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 175174 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 179363 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 179363 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 179363 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 213088 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 213088 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 161699 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 161699 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 91348 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 91348 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 126651 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 126651 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 126651 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 92988 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 92988 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 8438 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 8438 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 8438 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 8438 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 91526 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 91526 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 83319 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 83319 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 84090 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 84090 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 145440 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 145440 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 88934 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 88934 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 88940 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 88940 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 88940 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 127039 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 127039 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 108362 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 108362 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 188166 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 188166 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 83962 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 83962 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 83962 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 210840 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 210840 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 65316 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 65316 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 175130 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 175130 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 83290 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 83290 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 145441 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 145441 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 210742 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 210742 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 147785 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 147785 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 212820 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 212820 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 63208 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 63208 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 63208 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 9947 58 None -21 31 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 9947 58 None -21 31 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 9947 58 None -21 31 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 9947 58 None -21 31 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 9947 58 None -21 31 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 7581 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 7581 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 7581 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 7581 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 7581 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 204150 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 204150 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 194908 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 194908 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 194908 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 200078 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 200078 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 200078 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 186674 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 186674 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 187869 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 187869 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 20908 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 20908 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 20908 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 130784 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 130784 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 74201 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 74201 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 74201 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 101013 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 101013 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 64938 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 64938 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 205156 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 205156 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 75941 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 75941 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 16306 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 16306 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 7704 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 7704 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 7704 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 7704 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 7704 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 107825 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 107825 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 187574 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 187574 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 179487 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 179487 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 91893 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 91893 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 19714 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 19714 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 19714 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 19714 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 122562 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 122562 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 114398 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 114398 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 117967 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 117967 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 203404 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 203404 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 102780 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 102780 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 102780 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 103064 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 103064 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 103064 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 200093 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 200093 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 200093 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 7581 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 7581 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 7581 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 7581 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 7581 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 200076 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 200076 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 210755 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 210755 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 75949 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 75949 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 208591 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 208591 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 183187 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 183187 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 183187 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 177223 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 177223 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 91458 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 91458 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 185075 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 185075 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 185075 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 187759 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 187759 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 18625 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 18625 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 18625 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 19110 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 19110 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 19110 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 130789 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 130789 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 91517 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 91517 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 7581 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 7581 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 7581 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 7581 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 7581 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 7741 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 7741 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 7741 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 7741 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 7741 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 9641 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 9641 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 9641 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 9641 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 9641 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 116133 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 116133 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 20812 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 20812 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 20812 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 90574 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 90574 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 166080 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 166080 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 108928 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 108928 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 18687 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 18687 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 18687 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 18623 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 18623 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 18623 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 109594 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 109594 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 77343 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 77343 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 75941 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 75941 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 213526 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 213526 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 213526 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 86313 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 86313 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 185071 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 185071 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 185071 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 190407 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 190407 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 190407 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 130786 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 130786 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 93729 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 93729 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 110564 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 180840 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 180840 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 19105 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 19105 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 19105 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 111235 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 111235 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 46813 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 46813 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 7191 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 7191 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 7191 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 7191 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 7191 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 212292 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 212292 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 212292 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 193699 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 193699 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 193699 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 116122 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 116122 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 10636 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 10636 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 10636 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 177185 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 177185 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 111235 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 111235 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 202856 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 202856 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 202856 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 194239 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 194239 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 75783 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 75783 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 64320 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 64320 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 198939 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 198939 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 81250 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 81250 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 81250 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 176306 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 176306 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 167919 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 167919 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 167919 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 167029 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 167029 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 18665 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 18665 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 18665 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 105120 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 105120 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 83307 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 83307 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 83531 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 83531 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 83751 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 83751 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 176658 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 176658 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 168225 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 168225 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 11938 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 11938 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 148480 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 148480 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 148480 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 18661 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 18661 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 18661 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 106401 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 106401 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 140315 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 140315 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 119553 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 119553 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 119553 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 86312 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 86312 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 91063 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 91063 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 9957 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 9957 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 9957 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 9957 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 9957 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 194909 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 194909 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 194909 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 207222 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 207222 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 153199 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 153199 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 87206 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 87206 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 207222 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 207222 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 79461 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 79461 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 79461 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 118078 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 118078 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 116130 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 116130 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 200592 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 143415 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 143415 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 116124 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 116124 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 116128 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 116128 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 91425 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 91425 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 65319 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 65319 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 122552 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 122552 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 68590 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 68590 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 183421 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 183421 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 183421 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 116120 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 116120 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 65291 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 65291 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 91064 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 91064 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 18619 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 18619 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 18619 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 94760 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 94760 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 142928 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 142928 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 156887 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 156887 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 93580 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 93580 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 157449 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 157449 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 83011 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 83011 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 81231 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 81231 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 81231 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 167908 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 167908 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 167908 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 19168 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 19168 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 19168 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 109423 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 109423 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 77893 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 77893 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 130787 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 130787 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 90569 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 90569 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 170636 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 170636 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 92998 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 92998 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 127036 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 127036 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 19191 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 19191 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 19191 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 105714 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 105714 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 20899 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 20899 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 20899 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 167871 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 167871 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 167871 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 183189 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 183189 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 183189 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 163736 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 163736 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 171655 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 171655 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 194575 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 194575 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 194575 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 168229 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 168229 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 144902 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 144902 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 100890 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 100890 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 183377 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 183377 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 183377 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 194238 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 194238 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 178107 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 178107 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 163482 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 163482 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 25268 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 25268 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 86234 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 86234 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 100888 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 100888 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 161739 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 161739 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 185061 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 185061 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 185061 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 168385 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 168385 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 199852 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 199852 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 7253 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 7253 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 7253 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 7253 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 167750 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 167750 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 167750 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 181490 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 181490 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 7581 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 7581 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 7581 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 7581 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 7581 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 187758 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 187758 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 18685 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 18685 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 18685 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 179562 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 179562 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 214458 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 214458 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 7706 68 None -18 72 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 7706 68 None -18 72 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 7706 68 None -18 72 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 7706 68 None -18 72 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 7706 68 None -18 72 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
155556290 183235 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 183235 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 183235 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 81228 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 81228 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 81228 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 122556 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 122556 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 78806 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 78806 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 210749 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 210749 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 185020 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 185020 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 185020 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 187764 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 187764 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 183543 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 183543 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 20893 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 20893 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 20893 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 7581 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 7581 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 7581 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 7581 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 7581 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 113798 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 113798 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 16039 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 16039 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 11605 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 11605 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 188152 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 188152 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 106286 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 106286 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 65285 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 65285 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 109116 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 109116 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 127136 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 127136 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 130785 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 130785 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 7581 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 7581 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 7581 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 7581 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 7581 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 99308 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 99308 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 194210 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 194210 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 16306 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 16306 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 117343 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 117343 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 165297 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 165297 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 185039 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 185039 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 185039 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 20911 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 20911 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 20911 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 8963 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 8963 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 8963 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 8963 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 8963 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 7581 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 7581 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 7581 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 7581 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 7581 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 210362 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 210362 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 9905 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 9905 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 9905 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 9905 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 9905 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 167954 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 167954 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 167954 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 18659 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 18659 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 18659 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 86426 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 86426 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 53018 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 53018 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 65296 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 65296 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 19112 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 19112 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 19112 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 183308 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 183308 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 183308 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 81229 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 81229 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 81229 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 103554 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 103554 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 92973 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 92973 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 127627 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 127627 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 72761 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 72761 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 19074 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 19074 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 19074 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 208580 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 208580 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 7581 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 7581 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 7581 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 7581 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 7581 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 16167 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 16167 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 116117 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 116117 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 19067 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 19067 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 19067 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 113230 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 113230 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 113230 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 122777 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 122777 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 198279 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 198279 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 210625 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 210625 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 65292 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 65292 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 143160 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 143160 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 9753 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 9753 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 9753 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 9753 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 9753 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 9266 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 9266 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 9266 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 9266 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 9266 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 175869 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 175869 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 44656 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 44656 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 7189 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 7189 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 7189 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 7189 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 7189 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 85186 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 85186 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 85186 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 94094 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 94094 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 107313 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 107313 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 107313 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 175606 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 175606 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 47471 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 47471 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 7450 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 7450 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 7450 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 7450 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 7450 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 96590 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 96590 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 74543 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 74543 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 210521 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 210521 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 147427 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 147427 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 65298 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 65298 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 178994 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 178994 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 83167 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 83167 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 83832 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 83832 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 147493 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 147493 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 46576 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 46576 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 18800 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 18800 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 18800 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 143345 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 143345 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 11994 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 11994 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 93779 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 93779 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 81550 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 81550 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 82796 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 82796 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 84091 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 84091 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 65546 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 65546 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 127507 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 127507 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 165515 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 165515 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 107345 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 107345 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 183465 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 183465 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 183465 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 107824 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 107824 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 91431 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 91431 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 194659 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 194659 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 194659 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 7581 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 7581 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 7581 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 7581 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 7581 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 81670 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 81670 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 20808 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 20808 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 20808 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 199993 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 199993 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 11874 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 11874 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 164681 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 164681 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 8215 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 8215 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 8215 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 8215 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 8215 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 143324 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 143324 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 100843 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 100843 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 9281 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 9281 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 9281 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 9281 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 187728 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 187728 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 18682 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 18682 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 18682 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 187944 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 187944 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 179513 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 179513 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 130781 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 130781 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 91794 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 91794 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 19100 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 19100 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 19100 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 183236 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 183236 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 183236 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 189690 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 189690 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 91516 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 91516 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 7581 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 7581 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 7581 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 7581 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 7581 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 90582 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 90582 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 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
1213 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
2725 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
33036 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
4411 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
616 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
6976 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
716121 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C nan
155528270 183170 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 183170 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 183170 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 19106 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 19106 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 19106 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 187880 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 187880 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 65287 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 65287 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 8840 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 8840 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 8840 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 176888 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 176888 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 7581 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 7581 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 7581 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 7581 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 7581 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 19098 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 19098 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 19098 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 94090 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 94090 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 7736 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 7736 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 7736 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 7736 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 7736 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 122563 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 122563 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 177810 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 177810 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 7253 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 7253 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 7253 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 7253 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 7253 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 7253 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 7253 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 7253 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 65818 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 65818 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 122561 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 122561 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 164052 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 164052 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 86429 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 86429 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 100844 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 100844 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 111552 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 111552 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 167824 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 167824 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 167824 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 167938 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 167938 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 167938 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 96572 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 96572 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 182065 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 182065 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 7581 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 7581 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 7581 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 7581 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 7581 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 75941 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 75941 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 68587 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 68587 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 127746 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 127746 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 49556 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 49556 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 200564 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 83227 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 83227 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 221307 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 198813 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 198813 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 125837 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 125837 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 74701 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 74701 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 48748 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 48748 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 19530 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 19530 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 183220 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 183220 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 183220 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 96576 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 96576 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 91404 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 91404 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 184105 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 184105 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 144936 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 144936 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 142479 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 142479 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 91543 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 91543 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 91527 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 91527 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 211182 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 211182 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 94093 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 94093 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 201007 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 100764 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 100764 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 171843 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 171843 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 101654 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 101654 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 194632 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 194632 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 194632 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 176337 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 176337 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 182403 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 182403 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 189273 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 189273 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 183032 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 183032 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 183032 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 83961 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 83961 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 83961 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 91430 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 91430 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 168394 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 168394 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 9288 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 9288 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 9288 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 90147 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 90147 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 19110 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 19110 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 19110 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 175656 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 175656 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 175656 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 210856 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 210856 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 167983 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 167983 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 167983 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 7581 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 7581 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 7581 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 7581 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 7581 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 142479 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 142479 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 79617 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 79617 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 146902 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 146902 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 147251 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 147251 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 162585 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 162585 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 162585 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 7239 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 7239 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 7239 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 190424 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 190424 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 190424 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 208775 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 208775 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 10519 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 10519 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 10519 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 10519 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 10519 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 10519 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 65963 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 65963 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 185115 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 185115 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 185115 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 122559 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 122559 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 85390 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 85390 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 167799 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 167799 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 167799 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 7581 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 7581 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 7581 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 7581 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 7581 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 183188 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 183188 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 183188 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 7581 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 7581 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 7581 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 7581 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 7581 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 105670 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 105670 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 15497 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 15497 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 78945 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 78945 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 175487 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 175487 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 189391 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 189391 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 130783 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 130783 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 10636 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 10636 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 10636 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 195304 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 195304 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 195304 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 183079 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 183079 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 183079 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 10636 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 10636 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 10636 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 108952 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 108952 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 7581 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 7581 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 7581 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 7581 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 7581 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 190678 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 190678 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 7092 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 7092 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 7092 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 7092 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 7092 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 7092 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 7092 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 7092 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 183452 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 183452 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 183452 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 18690 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 18690 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 18690 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 93730 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 93730 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 162891 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 162891 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 189312 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 189312 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 20903 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 20903 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 20903 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 155025 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 155025 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 211670 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 211670 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 211670 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 81479 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 81479 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 210723 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 210723 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 213701 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 213701 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 213701 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 65299 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 65299 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 66206 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 66206 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 185086 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 185086 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 185086 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 113639 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 113639 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 203176 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 203176 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 177249 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 177249 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 11633 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 11633 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 183188 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 183188 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 183188 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 165272 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 165272 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 16358 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 16358 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 16358 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 7186 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 7186 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 7186 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 7186 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 7186 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 209886 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 209886 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 209886 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 209886 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 209886 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 209886 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7581 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 7581 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 7581 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 7581 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 7581 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 190406 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 190406 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 190406 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 11809 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 11809 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 11809 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 167929 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 167929 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 167929 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 214330 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 214330 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 200076 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 200076 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 195748 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 195748 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 195748 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 176277 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 176277 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 65293 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 65293 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 183865 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 183865 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 10614 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 10614 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 10614 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 10614 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 10614 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 20814 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 20814 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 20814 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 109665 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 109665 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 109665 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 65317 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 65317 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 91498 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 91498 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 91892 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 91892 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 103585 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 103585 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 130767 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 130767 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 201237 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 10869 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 10869 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 10869 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 10869 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 10869 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 205537 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 205537 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 183190 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 183190 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 183190 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 126011 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 126011 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 79553 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 79553 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 147058 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 147058 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 148063 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 148063 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 91138 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 91138 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 81218 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 81218 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 146942 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 146942 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 220996 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 221094 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 197460 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 197460 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 198368 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 198368 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 198838 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 198838 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 198857 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 198857 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 125844 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 125844 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 212616 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 212616 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 177040 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 177040 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 11996 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 11996 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 115377 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 115377 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 31833 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 31833 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 21922 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 21922 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 7581 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 7581 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 7581 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 7581 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 7581 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 63316 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 63316 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 63316 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 23471 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 23471 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 66451 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 66451 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 162981 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 162981 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 19107 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 19107 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 19107 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 101014 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 101014 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 93734 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 93734 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 83959 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 83959 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 83959 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 83959 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 83959 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 83959 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 22348 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 22348 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 22348 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 9793 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 9793 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 9793 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 19109 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 19109 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 19109 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 190037 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 190037 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 185027 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 185027 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 185027 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 185044 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 185044 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 185044 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 86902 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 86902 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 143984 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 143984 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 18644 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 18644 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 18644 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 101892 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 101892 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 175893 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 175893 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 66227 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 66227 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 188537 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 188537 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 18689 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 18689 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 18689 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 185102 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 185102 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 185102 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 210753 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 212530 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 212530 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 165271 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 165271 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 195346 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 195346 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 195346 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 102780 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 102780 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 102780 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 18684 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 18684 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 18684 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 18625 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 18625 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 18625 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 102780 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 102780 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 102780 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 102780 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 102780 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 102780 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 103343 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 103343 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 116116 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 116116 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 203356 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 203356 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 8439 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 8439 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 8439 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 8439 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 8439 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 7581 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 7581 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 7581 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 7581 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 7581 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 65288 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 65288 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 200078 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 200078 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 200078 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 17188 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 17188 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 178577 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 178577 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 183126 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 183126 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 183126 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 189449 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 189449 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 103585 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 103585 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 167799 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 167799 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 167799 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 195498 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 195498 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 195498 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 20907 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 20907 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 20907 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 210473 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 210473 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 163778 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 163778 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 167799 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 167799 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 167799 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 75443 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 75443 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 93778 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 93778 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 175183 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 175183 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 82770 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 82770 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 83022 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 83022 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 83049 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 83049 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 83479 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 83479 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 146969 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 146969 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 64939 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 64939 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 10869 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 10869 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 10869 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 10869 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 10869 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 20291 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 20291 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 20291 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 33269 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 33269 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 212905 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 212905 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 10869 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 10869 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 10869 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 10869 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 10869 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 82711 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 82711 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 100076 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 100076 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 205866 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 205866 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 113755 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 113755 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 17068 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 17068 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 94305 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 94305 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 186639 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 186639 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 15497 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 15497 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 182621 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 182621 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 7736 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 7736 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 7736 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 7736 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 7736 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 210630 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 210630 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 116118 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 116118 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 86428 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 86428 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 96578 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 96578 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 91925 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 91925 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 116132 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 116132 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 46689 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 46689 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 20811 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 20811 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 20811 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 18620 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 18620 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 18620 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 18620 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 183318 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 183318 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 183318 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 185078 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 185078 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 185078 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 190453 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 190453 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 190453 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 167755 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 167755 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 167755 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 65855 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 65855 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 127580 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 127580 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 167755 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 167755 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 167755 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 83955 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 83955 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 83955 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 183649 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 183649 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 91534 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 91534 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 203570 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 203570 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 24381 0 None -1445 26 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 24381 0 None -1445 26 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 9688 112 None -27 65 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 9688 112 None -27 65 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 9688 112 None -27 65 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 9688 112 None -27 65 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
16125570 149094 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 149094 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 163930 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 163930 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 208207 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 208207 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 93574 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 93574 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 65300 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 65300 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 184416 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 184416 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 210753 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 185046 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 185046 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 185046 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 185066 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 185066 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 185066 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 204461 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 204461 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 190450 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 190450 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 190450 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 7252 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 7252 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 7252 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 195327 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 195327 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 195327 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 186822 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 186822 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 187549 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 187549 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 185060 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 185060 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 185060 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 168003 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 168003 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 168003 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 19111 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 19111 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 19111 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 9956 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 9956 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 9956 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 9956 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 9956 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 19099 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 19099 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 19099 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 210528 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 210528 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 99013 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 99013 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 66453 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 66453 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 83958 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 83958 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 83958 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 16167 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 16167 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 91473 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 91473 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 116129 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 116129 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 15962 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 15962 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 100987 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 100987 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 20807 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 20807 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 20807 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 65294 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 65294 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 210775 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 210775 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 8083 62 None -11 50 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 8083 62 None -11 50 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 8083 62 None -11 50 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 8083 62 None -11 50 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 8083 62 None -11 50 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 119562 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 119562 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 119562 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 176470 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 176470 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 8816 69 None -32 39 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 8816 69 None -32 39 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 8816 69 None -32 39 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 176743 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 176743 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 11798 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 11798 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 12226 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 12226 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 7581 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 7581 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 7581 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 7581 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 7581 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 182928 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 182928 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 182928 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 182928 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 93731 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 93731 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 182049 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 182049 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 91424 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 91424 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 108858 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 108858 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 45103 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 45103 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 8706 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 8706 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 8706 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 8706 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 8706 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 8706 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 122551 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 122551 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 210808 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 210808 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 195281 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 195281 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 195281 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 8171 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 8171 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 8171 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 8171 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 8171 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 21188 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 21188 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 64666 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 64666 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 205151 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 205151 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 164288 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 164288 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 93732 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 93732 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 65545 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 65545 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 183266 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 183266 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 183266 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 9281 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 9281 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 9281 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 9281 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 195321 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 195321 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 195321 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 189716 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 189716 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 18807 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 18807 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 18807 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 101037 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 101037 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 24758 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 24758 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 24758 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 74403 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 74403 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 27397 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 27397 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 195894 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 195894 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 210836 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 210836 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 186581 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 186581 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 185054 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 185054 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 185054 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 77048 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 77048 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 83966 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 83966 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 83966 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 172347 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 172347 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 65301 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 65301 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 205863 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 205863 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 105252 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 105252 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 7581 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 7581 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 7581 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 7581 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 7581 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 9281 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 9281 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 9281 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 9281 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 10409 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 10409 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 10409 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 10409 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 10409 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 10229 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 10229 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 10229 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 10229 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 10229 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 10633 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 10633 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 10633 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 10633 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 10633 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 10633 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 10765 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 10765 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 10765 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 10765 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 10765 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 28477 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 28477 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 10465 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 10465 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 10465 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 10465 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 10465 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 10465 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 10766 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 10766 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 10766 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 10766 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 10766 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 119570 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 119570 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 7450 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 7450 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 7450 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 7450 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 7450 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 19504 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 19504 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 19504 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 19530 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 19530 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 7698 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 7698 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 7698 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 6900 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 6900 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 6900 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 6900 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 6900 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 6900 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 6900 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 6900 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 9525 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 9525 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 9525 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 10855 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 10855 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 10855 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 7450 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 7450 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 7450 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 7450 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 7450 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 7520 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 7520 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 7519 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 7519 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 7519 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 7519 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 7519 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 7519 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 8815 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 8815 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 8815 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 10575 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 10575 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 10465 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 10465 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 10465 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 10465 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 10465 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 10465 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 10465 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 10465 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 10465 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 10465 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 10465 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 10465 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 8617 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 8617 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 8617 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 10765 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 10765 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 10765 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 10765 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 10765 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 10853 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 10853 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 10853 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 10766 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 10766 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 10766 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 10766 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 10766 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 7128 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 7128 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 6900 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 6900 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 6900 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 6900 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 6900 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 6900 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 6900 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 6900 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 214820 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 214820 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 214820 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 214820 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 214820 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 214820 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 222816 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 214820 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 214820 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 214820 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 94799 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 94799 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 214820 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 214820 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 214820 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 8843 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 8843 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 8843 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 8843 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 8843 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 214820 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 214820 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 214820 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 222816 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 6904 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 6904 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 6904 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 214820 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 214820 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 214820 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 8843 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 8843 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 8843 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 8843 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 8843 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 6904 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 6904 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 6904 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 6904 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 6904 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 6904 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 9753 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 9753 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 9753 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 9753 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 9753 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 6904 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 6904 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 6904 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 222741 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 9753 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 9753 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 9753 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 9753 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 9753 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 214820 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 214820 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 214820 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 214820 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 214820 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 214820 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 223007 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 6904 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 6904 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 6904 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 214820 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 214820 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 214820 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 214820 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 214820 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 214820 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 222741 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 10377 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 10377 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 223007 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 155639 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 155639 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 8196 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 8196 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 8196 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 8196 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 8196 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 7450 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 7450 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 7450 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 7450 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 7450 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 9960 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 9960 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 9960 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 9960 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 9960 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 8703 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 8703 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 8703 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 10711 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 10711 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 10711 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 10711 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 10711 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 10711 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 222817 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 8439 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 8439 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 8439 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 8439 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 8439 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 10632 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 10632 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 10632 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 10632 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 10632 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 10632 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 15756 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 15756 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 222818 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 222818 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 224111 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 6928 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 6928 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 6928 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 6928 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 7188 115 3H-QNB -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 7188 115 3H-QNB -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 7188 115 3H-QNB -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 7188 115 3H-QNB -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 7188 115 3H-QNB -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
141 8209 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 8209 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 8209 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 8209 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 8622 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 8622 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 8622 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 8692 93 3H-QNB -154 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-QNB -154 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-QNB -154 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-QNB -154 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-QNB -154 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3294 8787 111 3H-NMS -14454 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 3H-NMS -14454 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 3H-NMS -14454 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 3H-NMS -14454 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 3H-NMS -14454 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1588 9105 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 9105 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 9105 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 9105 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 9105 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 9368 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 9368 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 9368 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 9368 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 9368 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 9368 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 9368 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 9368 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 9368 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 9368 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 9637 0 3H-QNB -32 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 3H-QNB -32 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 3H-QNB -32 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
119570 9933 96 3H-QNB -4570 39 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 9933 96 3H-QNB -4570 39 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 9933 96 3H-QNB -4570 39 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 9933 96 3H-QNB -4570 39 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 9933 96 3H-QNB -4570 39 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 10030 77 3H-QNB -81 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-QNB -81 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-QNB -81 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-QNB -81 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-QNB -81 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2389 10104 118 3H-QNB -602 66 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 10104 118 3H-QNB -602 66 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 10104 118 3H-QNB -602 66 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 10104 118 3H-QNB -602 66 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 10104 118 3H-QNB -602 66 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 10237 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 10237 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 10237 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 10237 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 10576 49 3H-NMS -4168 27 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 10576 49 3H-NMS -4168 27 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 10576 49 3H-NMS -4168 27 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 10625 55 3H-QNB -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 10625 55 3H-QNB -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 10625 55 3H-QNB -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 10625 55 3H-QNB -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 10625 55 3H-QNB -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
185 10778 60 3H-QNB -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 10778 60 3H-QNB -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 10778 60 3H-QNB -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 10778 60 3H-QNB -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
2865 10915 73 3H-QNB -812 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-QNB -812 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-QNB -812 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-QNB -812 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-QNB -812 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
103 10925 61 3H-QNB -144 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-QNB -144 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-QNB -144 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-QNB -144 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-QNB -144 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
10297 33885 30 3H-QNB -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 33885 30 3H-QNB -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
15387 52596 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 52596 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 62359 119 3H-QNB -42657 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-QNB -42657 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1979 84101 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 84101 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 106158 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 106158 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 106158 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 106743 83 3H-QNB -288 28 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 106743 83 3H-QNB -288 28 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 118369 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 118369 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 126303 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 126303 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 140299 14 3H-QNB -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 140299 14 3H-QNB -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
5280343 195054 124 3H-QNB -147 31 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 195054 124 3H-QNB -147 31 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 195054 124 3H-QNB -147 31 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 209053 22 3H-QNB -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 209053 22 3H-QNB -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 209053 22 3H-QNB -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
5281600 209804 92 3H-QNB -275 32 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 209804 92 3H-QNB -275 32 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 209845 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 209845 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 210262 15 3H-4-DAMP -3 36 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 210262 15 3H-4-DAMP -3 36 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 210262 15 3H-4-DAMP -3 36 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 211466 20 3H-QNB -52 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 211466 20 3H-QNB -52 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
5311189 211620 11 3H-QNB -112 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 211620 11 3H-QNB -112 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
4158 212120 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 212120 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 212120 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 212280 72 3H-QNB -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 212280 72 3H-QNB -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 212280 72 3H-QNB -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
3337 213146 27 3H-QNB -158 40 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 213146 27 3H-QNB -158 40 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 213146 27 3H-QNB -158 40 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 213146 27 3H-QNB -158 40 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 213146 27 3H-QNB -158 40 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 213445 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 213445 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 214288 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 214288 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 222732 0 3H-QNB -141253 59 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
5831 222742 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 222742 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 222758 0 3H-QNB -13182 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
40589 222923 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 222958 0 3H-QNB -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 222958 0 3H-QNB -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 223018 0 3H-QNB -38018 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
None 223085 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 223085 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 223086 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 223086 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 223090 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 223091 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 223092 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 223093 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 223094 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 223095 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 223096 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 223097 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 223104 0 3H-QNB -13 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 223105 0 3H-QNB -16 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 223106 0 3H-QNB -16 27 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 223107 0 3H-QNB -7 27 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 223108 0 3H-QNB -3 27 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 223109 0 3H-QNB -281 27 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 223110 0 3H-QNB -1 27 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 223229 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 223273 0 3H-NMS -1 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 399 7 4 5 1.8 CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O.C(CC(=O)O)C(=O)O.O None
214 10632 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 10632 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 10632 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 10632 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 10632 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 10632 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 9688 112 3H-QNB -27 65 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-QNB -27 65 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-QNB -27 65 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-QNB -27 65 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398737 7745 93 3H-NMS -10 90 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 7745 93 3H-NMSP -10 90 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-NMS -10 90 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-NMSP -10 90 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-NMS -10 90 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-NMSP -10 90 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-NMS -10 90 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-NMSP -10 90 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-NMS -10 90 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-NMSP -10 90 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
9905731 175287 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 175287 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 9281 12 3H-NMS -19 12 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 9281 12 3H-NMS -19 12 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 9281 12 3H-NMS -19 12 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 9281 12 3H-NMS -19 12 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
277 8083 62 3H-QNB -11 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 8083 62 3H-QNB -11 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 8083 62 3H-QNB -11 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 8083 62 3H-QNB -11 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 8083 62 3H-QNB -11 50 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
4919 213013 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 213013 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 7189 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 7189 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 7189 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 7189 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 7189 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 213526 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 213526 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 213526 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 9127 53 3H-QNB -19 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-QNB -19 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-QNB -19 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-QNB -19 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-QNB -19 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2200 9905 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 9905 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 9905 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 9905 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 9905 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 222817 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 91411 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 91411 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 9688 112 35S-GTPGammaS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 35S-GTPGammaS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 35S-GTPGammaS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 35S-GTPGammaS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2745 10633 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 10633 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 10633 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 10633 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 10633 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 10633 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 10594 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 10594 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 10594 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 10030 77 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135398745 9688 112 3H-NMS -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 9688 112 3H-QNB -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-NMS -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-QNB -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-NMS -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-QNB -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-NMS -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-QNB -27 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3947 213174 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 213174 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 10915 73 3H-QNB -812 53 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-QNB -812 53 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-QNB -812 53 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-QNB -812 53 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-QNB -812 53 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
68617 212306 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 212306 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 212306 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 9281 12 3H-NMS -66 12 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 9281 12 3H-NMS -66 12 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 9281 12 3H-NMS -66 12 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 9281 12 3H-NMS -66 12 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
135398745 9688 112 3H-NMS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 9688 112 3H-NMSP -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-NMS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-NMSP -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-NMS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-NMSP -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-NMS -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-NMSP -27 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2337 10030 77 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 10030 77 3H-NMS -257 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-NMS -257 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-NMS -257 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-NMS -257 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-QNB -81 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-NMS -257 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2200 9905 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 9905 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 9905 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 9905 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 9905 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 7745 93 3H-NMS -7 90 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 7745 93 3H-QNB -7 90 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-NMS -7 90 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-QNB -7 90 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-NMS -7 90 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-QNB -7 90 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-NMS -7 90 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-QNB -7 90 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-NMS -7 90 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-QNB -7 90 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
44431386 155804 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 155804 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 222817 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 9281 12 3H-NMS -66 12 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 9281 12 3H-NMS -66 12 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 9281 12 3H-NMS -66 12 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 9281 12 3H-NMS -66 12 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
10090005 222765 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 222817 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 8443 50 3H-QNB -407 65 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-QNB -407 65 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-QNB -407 65 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-QNB -407 65 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-QNB -407 65 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1212 8443 50 3H-QNB -2884 65 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-QNB -2884 65 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-QNB -2884 65 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-QNB -2884 65 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-QNB -2884 65 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
100 10577 58 3H-QNB -8 54 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 10577 58 3H-QNB -8 54 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 10577 58 3H-QNB -8 54 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 10577 58 3H-QNB -8 54 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 10577 58 3H-QNB -8 54 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 223036 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 223036 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 9905 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 9905 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 9905 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 9905 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 9905 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 52596 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 52596 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 223154 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 9637 0 3H-QNB -32 36 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 3H-QNB -32 36 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 3H-QNB -32 36 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
2200 9905 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 9905 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 9905 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 9905 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 9905 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 223018 0 3H-QNB -38018 29 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
124226 8702 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 8702 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 223151 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 8692 93 3H-NMS -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 8692 93 3H-QNB -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-NMS -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-QNB -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-NMS -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-QNB -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-NMS -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-QNB -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-NMS -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-QNB -2344 85 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
11954259 222758 0 3H-QNB -13182 43 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
154734599 9281 12 3H-NMS -66 12 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 9281 12 3H-NMS -66 12 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 9281 12 3H-NMS -66 12 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 9281 12 3H-NMS -66 12 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
2200 9905 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 9905 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 9905 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 9905 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 9905 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 94758 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 94758 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 9905 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 9905 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 9905 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 9905 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 9905 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 10636 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 10636 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 10636 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 9831 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 9831 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 9831 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 9831 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 9831 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 174570 24 3H-QNB -5 44 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 174570 24 3H-QNB -5 44 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
209 9831 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 9831 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 9831 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 9831 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 9831 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 94092 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 94092 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 10030 77 3H-QNB -81 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-QNB -81 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-QNB -81 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-QNB -81 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-QNB -81 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
16362 9899 71 3H-QNB -10232 29 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 3H-QNB -10232 29 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 3H-QNB -10232 29 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 3H-QNB -10232 29 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 3H-QNB -10232 29 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
16362 9899 71 3H-QNB -562 29 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 3H-QNB -562 29 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 3H-QNB -562 29 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 3H-QNB -562 29 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 3H-QNB -562 29 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
154734599 9281 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 9281 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 9281 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 9281 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 214820 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 214820 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 214820 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 223007 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 94761 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 94761 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 214820 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 214820 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 214820 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 223035 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 6904 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 6904 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 6904 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 10633 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 10633 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 10633 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 10633 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 10633 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 10633 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 94796 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 94796 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 21270 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 21270 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 94797 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 94797 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 6904 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 6904 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 6904 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 152929 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 152929 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 10633 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 10633 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 10633 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 10633 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 10633 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 10633 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 7745 93 3H-QNB -10 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-QNB -10 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-QNB -10 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-QNB -10 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-QNB -10 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
44431367 94757 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 94757 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 94759 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 94759 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 222742 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 7707 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 7707 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 7707 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 7707 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 211184 53 3H-QNB -5 23 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 211184 53 3H-QNB -5 23 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 211184 53 3H-QNB -5 23 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
154734599 9281 12 3H-NMS -19 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 9281 12 3H-NMS -19 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 9281 12 3H-NMS -19 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 9281 12 3H-NMS -19 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
11976 7707 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 7707 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 7707 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 7707 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 84101 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 84101 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 9905 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 9905 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 9905 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 9905 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 9905 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 10636 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 10636 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 10636 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 222924 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 9905 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 9905 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 9905 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 9905 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 9905 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 8214 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 8214 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 8214 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 8214 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 8214 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 8214 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 94091 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 94091 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 222914 0 3H-QNB -2511 23 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
100 10577 58 3H-QNB -12 54 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 10577 58 3H-QNB -12 54 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 10577 58 3H-QNB -12 54 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 10577 58 3H-QNB -12 54 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 10577 58 3H-QNB -12 54 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7745 93 3H-QNB -10 90 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-QNB -10 90 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-QNB -10 90 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-QNB -10 90 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-QNB -10 90 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398745 9688 112 3H-NMS -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 9688 112 3H-QNB -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-NMS -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-QNB -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-NMS -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-QNB -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-NMS -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-QNB -16 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398737 7745 93 3H-QNB -7 90 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-QNB -7 90 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-QNB -7 90 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-QNB -7 90 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-QNB -7 90 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1613 9127 53 3H-QNB -70 44 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-QNB -70 44 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-QNB -70 44 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-QNB -70 44 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-QNB -70 44 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2435 10362 83 3H-QNB -5248 48 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 3H-QNB -5248 48 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 3H-QNB -5248 48 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 3H-QNB -5248 48 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 3H-QNB -5248 48 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2435 10362 83 3H-QNB -239 48 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 3H-QNB -239 48 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 3H-QNB -239 48 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 3H-QNB -239 48 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 3H-QNB -239 48 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
154734599 9281 12 3H-NMS -19 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 9281 12 3H-NMS -19 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 9281 12 3H-NMS -19 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 9281 12 3H-NMS -19 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
108107 86719 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 86719 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 86719 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 86719 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 223856 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 155800 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 155800 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 103585 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 103585 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 6904 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 6904 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 6904 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 7450 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 7450 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 7450 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 7450 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 7450 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 8703 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 8703 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 8703 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 9281 12 3H-NMS -66 12 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 9281 12 3H-NMS -66 12 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 9281 12 3H-NMS -66 12 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 9281 12 3H-NMS -66 12 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
154734599 9281 12 3H-PIRENZEPINE -66 12 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
327 9281 12 3H-PIRENZEPINE -66 12 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
4108 9281 12 3H-PIRENZEPINE -66 12 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
CHEMBL27673 9281 12 3H-PIRENZEPINE -66 12 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC None
62865 8057 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 8057 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 8057 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 8057 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 8057 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 9905 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 9905 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 9905 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 9905 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 9905 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 114308 20 3H-NMS -776 53 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 3H-NMS -776 53 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 3H-NMS -776 53 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 3H-NMS -776 53 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
3337 213146 27 3H-QNB -158 40 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 213146 27 3H-QNB -158 40 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 213146 27 3H-QNB -158 40 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 213146 27 3H-QNB -158 40 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 213146 27 3H-QNB -158 40 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 222880 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 223033 0 3H-NMS -3090 20 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 223209 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 10640 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 10640 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 10640 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 10640 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 10640 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 10640 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 10636 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 10636 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 10636 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 7189 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 7189 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 7189 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 7189 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 7189 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 10869 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 10869 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 10869 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 10869 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 10869 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 9127 53 3H-QNB -19 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-QNB -19 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-QNB -19 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-QNB -19 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-QNB -19 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2337 10030 77 3H-QNB -257 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-QNB -257 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-QNB -257 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-QNB -257 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-QNB -257 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
10938 8483 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 8483 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 8483 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 8483 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 7410 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 7410 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 7410 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 7410 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 7410 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 153199 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 153199 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 94760 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 94760 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 8442 26 3H-QNB -8 17 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 8442 26 3H-QNB -8 17 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 8442 26 3H-QNB -8 17 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
187 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7253 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 7253 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 7253 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 7253 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 10577 58 3H-QNB -8 54 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 10577 58 3H-QNB -8 54 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 10577 58 3H-QNB -8 54 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 10577 58 3H-QNB -8 54 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 10577 58 3H-QNB -8 54 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 9688 112 3H-QNB -16 65 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-QNB -16 65 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-QNB -16 65 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-QNB -16 65 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
7534 223152 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 223035 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 9905 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 9905 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 9905 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 9905 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 9905 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 9292 24 3H-QNB -134 67 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-QNB -134 67 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-QNB -134 67 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-QNB -134 67 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-QNB -134 67 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
242 7258 124 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 7258 124 3H-QNB -3388 51 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-QNB -3388 51 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-QNB -3388 51 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-QNB -3388 51 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-QNB -3388 51 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 7258 124 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-QNB -114 51 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2726 7706 68 3H-QNB -18 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-QNB -18 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-QNB -18 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-QNB -18 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-QNB -18 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1192 6935 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 6935 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 6935 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 8692 93 None -154 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 None -154 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 None -154 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 None -154 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 None -154 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1830 9368 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 9368 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 9368 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 9368 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 9368 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 10104 118 None -602 66 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 10104 118 None -602 66 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 10104 118 None -602 66 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 10104 118 None -602 66 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 10104 118 None -602 66 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 10915 73 None -812 53 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 None -812 53 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 None -812 53 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 None -812 53 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 None -812 53 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2448 106099 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 106099 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 222962 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 211405 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 211405 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 53018 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 53018 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 7258 124 None -114 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 None -114 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 None -114 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 None -114 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 None -114 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
66265 100788 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 100788 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 10578 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 10578 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 10578 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 10578 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 10578 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 167029 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 167029 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 46813 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 46813 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 7704 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 7704 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 7704 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 7704 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 7704 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 27105 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 27105 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 10362 83 None -239 48 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 None -239 48 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 None -239 48 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 None -239 48 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 None -239 48 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2812 11551 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 11551 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 9899 71 None -562 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 None -562 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 None -562 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 None -562 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 None -562 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
209 9831 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 9831 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 9831 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 9831 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 9831 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 10030 77 None -81 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 None -81 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 None -81 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 None -81 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 None -81 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
44431388 94094 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 94094 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 224490 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 9370 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 9370 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 9370 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 9370 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 9370 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 21240 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 21240 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 21240 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 212306 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 212306 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 212306 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 8841 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 8841 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 8841 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 9641 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 9641 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 9641 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 9641 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 9641 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 9637 0 3H-QNB -32 36 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 3H-QNB -32 36 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 3H-QNB -32 36 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
135398745 9688 112 3H-QNB -27 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-QNB -27 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-QNB -27 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-QNB -27 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
5831 222742 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 8253 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 8253 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 8253 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 8253 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 8253 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 222791 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 94090 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 94090 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 10915 73 3H-QNB -11481 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-QNB -11481 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-QNB -11481 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-QNB -11481 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-QNB -11481 53 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
73707487 223153 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 8443 50 None -407 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 None -407 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 None -407 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 None -407 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 None -407 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1209 8439 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 8439 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 8439 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 8439 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 8439 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 10632 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 10632 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 10632 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 10632 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 10632 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 10632 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 205863 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 205863 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 24758 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 24758 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 24758 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 182928 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 182928 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 182928 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 182928 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 22348 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 22348 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 22348 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 7186 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 7186 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 7186 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 7186 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 7186 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 213701 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 213701 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 213701 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 211670 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 211670 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 211670 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 10519 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 10519 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 10519 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 10519 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 10519 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 10519 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 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 7705 51 None -125 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(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6918558 21286 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 21286 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 95356 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 95356 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 95356 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 10633 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 10633 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 10633 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 10633 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 10633 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 10633 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 7191 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 7191 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 7191 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 7191 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 7191 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 212292 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 212292 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 212292 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 9947 58 None -21 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 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 9947 58 None -21 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 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 9947 58 None -21 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 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 9947 58 None -21 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 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 9947 58 None -21 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 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
12488 8438 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 8438 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 8438 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 8438 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 9310 43 None -22 56 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 9310 43 None -22 56 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 9310 43 None -22 56 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 9310 43 None -22 56 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 9310 43 None -22 56 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 211644 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 211644 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 211644 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 211644 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 8963 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 8963 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 8963 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 8963 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 8963 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 9905 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 9905 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 9905 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 9905 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 9905 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 8214 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 8214 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 8214 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 8214 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 8214 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 8214 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 211184 53 None -5 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 211184 53 None -5 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 211184 53 None -5 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
21855 91021 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 91021 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 85176 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 85176 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 7293 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 7293 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 7293 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 7293 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 7293 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 7727 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 7727 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 7727 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 7727 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 7727 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 8063 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 8063 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 8063 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 8063 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 8063 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 94093 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 94093 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 109635 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 109635 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 213174 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 213174 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 9127 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1427 8794 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 8794 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 8794 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 8794 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 8794 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 7706 68 3H-QNB -35 72 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-QNB -35 72 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-QNB -35 72 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-QNB -35 72 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-QNB -35 72 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
129989 7239 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 7239 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 7239 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 223037 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 7706 68 3H-QNB -18 72 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-QNB -18 72 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-QNB -18 72 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-QNB -18 72 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-QNB -18 72 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
3337 213146 27 3H-QNB -158 40 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 213146 27 3H-QNB -158 40 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 213146 27 3H-QNB -158 40 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 213146 27 3H-QNB -158 40 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 213146 27 3H-QNB -158 40 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 89183 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 89183 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 210358 29 None -1 12 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
CHEMBL668 210358 29 None -1 12 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
135398737 7745 93 3H-NMS -10 90 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 7745 93 3H-QNB -10 90 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-NMS -10 90 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-QNB -10 90 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-NMS -10 90 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-QNB -10 90 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-NMS -10 90 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-QNB -10 90 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-NMS -10 90 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-QNB -10 90 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1712 9270 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 9270 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 9270 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 9270 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 9270 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 9956 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 9956 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 9956 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 9956 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 9956 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 18620 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 18620 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 18620 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 18620 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 9688 112 None -27 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 None -27 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 None -27 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 None -27 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
103 10925 61 None -144 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 None -144 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 None -144 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 None -144 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 None -144 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
1427 8794 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 8794 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 8794 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 8794 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 8794 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 213013 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 213013 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 7706 68 None -18 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 None -18 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 None -18 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 None -18 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 None -18 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
3055 8215 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 8215 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 8215 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 8215 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 8215 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 8253 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 8253 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 8253 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 8253 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 8253 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 9641 38 None -4 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 9641 38 None -4 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 9641 38 None -4 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 9641 38 None -4 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 9641 38 None -4 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
6075 156887 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 156887 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 193699 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 193699 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 193699 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 48495 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 48495 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 213526 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 213526 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 213526 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 7741 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 7741 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 7741 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 7741 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 7741 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 8171 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 8171 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 8171 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 8171 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 8171 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 8057 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 8057 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 8057 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 8057 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 8057 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 10640 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 10640 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 10640 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 10640 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 10640 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 10640 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 9905 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 9905 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 9905 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 9905 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 9905 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 7745 93 None -10 90 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 None -10 90 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 None -10 90 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 None -10 90 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 None -10 90 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
100 10577 58 None -8 54 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 10577 58 None -8 54 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 10577 58 None -8 54 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 10577 58 None -8 54 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 10577 58 None -8 54 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 101654 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 101654 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 223153 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 10869 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 10869 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 10869 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 10869 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 10869 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 7189 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 7189 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 7189 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 7189 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 7189 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 213013 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 213013 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 10030 77 3H-NMS -81 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-NMS -81 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-NMS -81 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-NMS -81 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-NMS -81 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1353 8692 93 3H-QNB -2344 85 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-QNB -2344 85 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-QNB -2344 85 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-QNB -2344 85 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-QNB -2344 85 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2448 106099 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 106099 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 106099 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 106099 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 10925 61 3H-QNB -60 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-QNB -60 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-QNB -60 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-QNB -60 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-QNB -60 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2200 9905 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 9905 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 9905 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 9905 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 9905 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 10925 61 3H-QNB -144 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-QNB -144 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-QNB -144 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-QNB -144 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-QNB -144 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
208 9638 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 9638 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 9638 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 10409 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 10409 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 10409 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 10409 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 10409 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 8083 62 None -11 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 8083 62 None -11 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 8083 62 None -11 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 8083 62 None -11 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 8083 62 None -11 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
26987 7736 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 7736 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 7736 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 7736 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 7736 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 10614 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 10614 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 10614 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 10614 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 10614 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 162300 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 162300 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 85186 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 85186 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 85186 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 9957 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 9957 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 9957 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 9957 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 9957 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 10614 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 10614 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 10614 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 10614 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 10614 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 9266 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 9266 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 9266 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 9266 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 9266 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8704 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 8704 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 8704 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 8704 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 8704 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 7384 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 7384 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 7384 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 7384 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 7384 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 7384 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 193699 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 193699 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 193699 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 9905 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 9905 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 9905 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 9905 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 9905 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 222817 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 10104 118 3H-QNB -22908 66 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 10104 118 3H-QNB -22908 66 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 10104 118 3H-QNB -22908 66 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 10104 118 3H-QNB -22908 66 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 10104 118 3H-QNB -22908 66 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 9270 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 9270 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 9270 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 9270 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 9270 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 9753 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 9753 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 9753 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 9753 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 9753 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 8196 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 8196 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 8196 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 8196 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 8196 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 9753 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 9753 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 9753 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 9753 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 9753 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 224507 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 62426 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 62426 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 62426 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 62426 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 19530 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 19530 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 214820 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 214820 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 214820 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 7739 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 7739 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 7739 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 7739 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 7739 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 7739 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 8608 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 8608 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 8608 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 8608 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 8608 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 8608 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 62426 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 62426 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 62426 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 62426 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 10095 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 10095 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 10095 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 10095 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 10095 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 29953 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 29953 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 214820 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 214820 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 214820 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 9270 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 9270 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 9270 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 9270 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 9270 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 222817 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 222817 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 8816 69 3H-QNB -32 39 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 8816 69 3H-QNB -32 39 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 8816 69 3H-QNB -32 39 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 213526 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 213526 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 213526 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 10339 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 10339 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 10339 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 10095 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 10095 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 10095 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 10095 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 10095 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 7670 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 7670 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 7670 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 7670 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 7670 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 9960 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 9960 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 9960 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 9960 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 9960 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 7049 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 10711 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 10711 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 10711 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 10711 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 10711 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 10711 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 10711 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 10711 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 10711 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 10711 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 10711 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 10711 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 10596 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 9611 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 9611 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 9611 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 9611 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 9611 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 9611 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7581 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 7410 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 7410 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 7410 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 7410 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 7410 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 7410 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 7410 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 7410 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 7410 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 7410 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 9752 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 9752 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 9752 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 9752 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 9897 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 9897 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 9897 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 9897 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 9897 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 9897 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 9897 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 9897 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 9897 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 9897 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 9751 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 9751 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 9751 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 9751 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 9751 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 9751 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 7253 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 7253 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 7253 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 7253 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 7253 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 7253 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 7253 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 7253 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 7253 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 7253 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 7253 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 7253 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 9748 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 9748 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 9748 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 10802 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 10802 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 10802 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 8672 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 8672 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 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
154734599 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
154734599 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
154734599 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9029489
154734599 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
327 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
327 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
327 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
327 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9029489
327 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
4108 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
4108 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
4108 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
4108 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9029489
4108 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
CHEMBL27673 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 1994002
CHEMBL27673 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 2704370
CHEMBL27673 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 8759038
CHEMBL27673 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9029489
CHEMBL27673 9281 12 None -19 12 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 582 29 4 6 7.2 COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC 9113359
2200 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 9905 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 10636 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 10636 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 10636 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 10640 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 10640 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 10640 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 10640 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 10640 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 10640 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 8706 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 8706 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 8706 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 8706 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 8706 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 8706 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 8706 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 8706 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 8706 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 7092 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 7092 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 7092 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 7092 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 7239 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 7239 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 7239 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 7239 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 7239 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 7239 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 10869 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 10869 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 10869 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 10869 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 10869 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 10869 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 10869 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 10869 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 10869 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 10869 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 10869 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 10869 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 10869 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 10869 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 10869 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 8248 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 8248 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 8248 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 10409 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 10409 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 10409 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 10409 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 10409 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 10409 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 10409 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 10409 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 10409 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 10409 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 7189 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 7189 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 7189 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 7189 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 7189 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 10706 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 10706 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 10706 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 10706 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 10614 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 9266 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 9266 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 9266 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 9266 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 9266 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 9753 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 9753 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 9753 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 9753 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 9753 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 9753 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 9753 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 9753 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 9753 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 9753 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8106 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 8196 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 8196 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 8196 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 8196 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 8196 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 6904 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 6904 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 6904 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 6904 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 6904 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 6904 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 10335 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 10335 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 10335 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 10335 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 10335 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 10335 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 10335 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 10335 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 8843 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 8843 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 8843 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 8843 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 8843 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 8843 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 8843 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 8843 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 8843 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 8843 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 8843 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 8843 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 8843 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 8843 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 8843 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 7739 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 7739 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 7739 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 7739 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 7739 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 7739 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 7089 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 7089 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 9355 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 9355 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 9355 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 9469 0 None -1122018 5 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10799315
313 9468 0 None -407 6 Human 6.0 pKi > 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7925952
134 9292 24 None -134 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 None -134 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 None -134 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 None -134 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 None -134 67 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
46780481 114308 20 None -776 53 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 None -776 53 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 None -776 53 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 None -776 53 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
3337 213146 27 None -158 40 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 213146 27 None -158 40 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 213146 27 None -158 40 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 213146 27 None -158 40 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 213146 27 None -158 40 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 222924 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 7707 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 7707 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 7707 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 7707 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 210371 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 210371 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 211405 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 211405 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 8483 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 8483 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 8483 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 8483 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 7581 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 7581 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 7581 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 7581 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 7581 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 9288 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 9288 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 9288 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 9312 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 9312 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 9312 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 9251 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 9251 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 9251 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 9251 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 9251 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 7043 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 7043 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 7043 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 7043 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 7043 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 7043 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 7252 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 7252 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 7252 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 9108 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 9108 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 9108 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 9108 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 9748 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 9748 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 9748 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 9905 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 9905 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 9905 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 9905 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 9905 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 10229 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 10229 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 10229 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 10229 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 10229 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 9616 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 9616 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 9616 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 8841 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 8841 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 8841 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 8841 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 8841 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 8841 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 8702 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 8702 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 8703 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 8703 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 8703 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 8703 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 8703 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 8703 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 8841 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 8841 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 8841 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 9618 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 9618 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 9821 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 9821 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 9821 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 9617 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 9617 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 8704 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 8704 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 8704 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 8704 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 8704 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 10377 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 10377 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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 7311 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