Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
129456 202706 11 None 8 2 Human 10.4 pEC50 = 10.4 Functional
In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by Muscarinic M2 receptor)In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by Muscarinic M2 receptor)
ChEMBL 179 1 0 4 0.8 Cc1noc(C2CN3CCC2C3)n1 10.1021/jm00083a016
CHEMBL92421 202706 11 None 8 2 Human 10.4 pEC50 = 10.4 Functional
In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by Muscarinic M2 receptor)In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by Muscarinic M2 receptor)
ChEMBL 179 1 0 4 0.8 Cc1noc(C2CN3CCC2C3)n1 10.1021/jm00083a016
10104167 1938 1 None -1 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 1938 1 None -1 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 1938 1 None -1 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL1223804 15737 0 None -251 5 Human 7.0 pEC50 = 7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
137630848 160313 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 160313 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 160313 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 213 3 0 3 1.5 C[N+]1(C)CCC(OCc2nccs2)C1 10.1021/acs.jmedchem.7b01113
10386 160365 10 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 160365 10 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 160365 10 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 180 3 1 1 1.6 C[N+](C)(C)CCc1cccc(O)c1 10.1021/acs.jmedchem.7b01113
2230 448 50 None 3 9 Human 5.0 pEC50 = 5 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1016/s0960-894x(98)00509-5
296 448 50 None 3 9 Human 5.0 pEC50 = 5 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1016/s0960-894x(98)00509-5
CHEMBL7303 448 50 None 3 9 Human 5.0 pEC50 = 5 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1016/s0960-894x(98)00509-5
DB04365 448 50 None 3 9 Human 5.0 pEC50 = 5 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1016/s0960-894x(98)00509-5
2551 755 22 None -2 12 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as induction of Galphaq/i5-mediated IP1 accumulation after 1 hr by HTRF assayAgonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as induction of Galphaq/i5-mediated IP1 accumulation after 1 hr by HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b01967
298 755 22 None -2 12 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as induction of Galphaq/i5-mediated IP1 accumulation after 1 hr by HTRF assayAgonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as induction of Galphaq/i5-mediated IP1 accumulation after 1 hr by HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b01967
488 755 22 None -2 12 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as induction of Galphaq/i5-mediated IP1 accumulation after 1 hr by HTRF assayAgonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as induction of Galphaq/i5-mediated IP1 accumulation after 1 hr by HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b01967
CHEMBL965 755 22 None -2 12 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as induction of Galphaq/i5-mediated IP1 accumulation after 1 hr by HTRF assayAgonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as induction of Galphaq/i5-mediated IP1 accumulation after 1 hr by HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b01967
DB00411 755 22 None -2 12 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as induction of Galphaq/i5-mediated IP1 accumulation after 1 hr by HTRF assayAgonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as induction of Galphaq/i5-mediated IP1 accumulation after 1 hr by HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b01967
49799920 10280 0 None -6 2 Human 6.0 pEC50 = 6.0 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CC[C@@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL1169506 10280 0 None -6 2 Human 6.0 pEC50 = 6.0 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CC[C@@H]1C2 10.1016/s0960-894x(98)00509-5
11120503 3968 0 None -16 2 Human 6.0 pEC50 = 6.0 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@@H]1CN2CC[C@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL100163 3968 0 None -16 2 Human 6.0 pEC50 = 6.0 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@@H]1CN2CC[C@H]1C2 10.1016/s0960-894x(98)00509-5
137629935 160217 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4060823 160217 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116342 160217 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
44329977 110709 0 None -10 2 Human 8.0 pEC50 = 8.0 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC1C2 10.1016/s0960-894x(98)00509-5
CHEMBL327269 110709 0 None -10 2 Human 8.0 pEC50 = 8.0 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC1C2 10.1016/s0960-894x(98)00509-5
44589681 184451 0 None -1 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at muscarinic M2 receptorAgonist activity at muscarinic M2 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 184451 0 None -1 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at muscarinic M2 receptorAgonist activity at muscarinic M2 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 186226 1 None -5 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at muscarinic M2 receptorAgonist activity at muscarinic M2 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 186226 1 None -5 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at muscarinic M2 receptorAgonist activity at muscarinic M2 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
2551 755 22 None -2 12 Human 7.0 pEC50 = 7.0 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00050a006
298 755 22 None -2 12 Human 7.0 pEC50 = 7.0 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00050a006
488 755 22 None -2 12 Human 7.0 pEC50 = 7.0 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00050a006
CHEMBL965 755 22 None -2 12 Human 7.0 pEC50 = 7.0 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00050a006
DB00411 755 22 None -2 12 Human 7.0 pEC50 = 7.0 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00050a006
10104047 21269 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 192 3 1 4 0.9 C=CCn1ncc(C2CCCNC2)n1 10.1021/jm00050a006
CHEMBL131777 21269 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 192 3 1 4 0.9 C=CCn1ncc(C2CCCNC2)n1 10.1021/jm00050a006
137629935 160217 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4060823 160217 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL4116342 160217 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
122191002 122859 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccccc1F 10.1016/j.bmcl.2015.08.011
CHEMBL3618445 122859 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccccc1F 10.1016/j.bmcl.2015.08.011
170332 160173 1 None -2 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 160173 1 None -2 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 160173 1 None -2 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
3652 3869 67 None -18 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
57 3869 67 None -18 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
60809 3869 67 None -18 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
CHEMBL21536 3869 67 None -18 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
DB15357 3869 67 None -18 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
44303017 196412 0 None -19 2 Human 5.9 pEC50 = 5.9 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 343 3 0 5 2.4 Clc1ccc(C#CCOc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
CHEMBL60101 196412 0 None -19 2 Human 5.9 pEC50 = 5.9 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 343 3 0 5 2.4 Clc1ccc(C#CCOc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
CHEMBL1223806 15739 0 None -158 5 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
45786849 157009 23 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 192 3 1 3 1.4 c1cncc(COC2CCCNC2)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4083241 157009 23 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 192 3 1 3 1.4 c1cncc(COC2CCCNC2)c1 10.1021/acs.jmedchem.7b01113
44330073 203951 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 327 3 0 5 3.1 C(#Cc1ccccc1)CSc1nsnc1[C@@H]1CN2CC[C@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL99884 203951 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 327 3 0 5 3.1 C(#Cc1ccccc1)CSc1nsnc1[C@@H]1CN2CC[C@H]1C2 10.1016/s0960-894x(98)00509-5
44209166 59052 0 None 7 2 Human 7.9 pEC50 = 7.9 Functional
In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by muscarinic acetylcholine receptor M2)In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by muscarinic acetylcholine receptor M2)
ChEMBL 193 1 0 4 1.0 Cc1noc(C2(C)CN3CCC2C3)n1 10.1021/jm00083a016
CHEMBL171721 59052 0 None 7 2 Human 7.9 pEC50 = 7.9 Functional
In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by muscarinic acetylcholine receptor M2)In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by muscarinic acetylcholine receptor M2)
ChEMBL 193 1 0 4 1.0 Cc1noc(C2(C)CN3CCC2C3)n1 10.1021/jm00083a016
44303408 197525 0 None -16 3 Human 5.8 pEC50 = 5.8 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 361 3 0 5 2.6 Fc1cc(Cl)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL60777 197525 0 None -16 3 Human 5.8 pEC50 = 5.8 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 361 3 0 5 2.6 Fc1cc(Cl)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
10451242 198688 0 None -218 3 Human 5.8 pEC50 = 5.8 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 361 3 0 5 2.8 Fc1cc(F)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL64029 198688 0 None -218 3 Human 5.8 pEC50 = 5.8 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 361 3 0 5 2.8 Fc1cc(F)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL3616500 122583 0 None -4 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 499 5 2 3 5.4 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C(F)(F)F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
89777356 155095 0 None -72 2 Human 5.8 pEC50 = 5.8 Functional
Activity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilizationActivity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 3 2 6 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4060475 155095 0 None -72 2 Human 5.8 pEC50 = 5.8 Functional
Activity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilizationActivity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 353 3 2 6 2.5 Cc1nnc2sc(C(=O)NC3CN(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
53385782 73762 0 None -56 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M2 receptor by calcium mobilization assayAgonist activity at human muscarinic M2 receptor by calcium mobilization assay
ChEMBL 399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024331 73762 0 None -56 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M2 receptor by calcium mobilization assayAgonist activity at human muscarinic M2 receptor by calcium mobilization assay
ChEMBL 399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
424727 160371 2 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 180 3 0 1 1.9 COc1ccccc1C[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL4095774 160371 2 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 180 3 0 1 1.9 COc1ccccc1C[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL4117601 160371 2 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 180 3 0 1 1.9 COc1ccccc1C[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
129456 202706 11 None 8 2 Human 7.7 pEC50 = 7.7 Functional
In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by Muscarinic M2 receptor)In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by Muscarinic M2 receptor)
ChEMBL 179 1 0 4 0.8 Cc1noc(C2CN3CCC2C3)n1 10.1021/jm00083a016
CHEMBL92421 202706 11 None 8 2 Human 7.7 pEC50 = 7.7 Functional
In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by Muscarinic M2 receptor)In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by Muscarinic M2 receptor)
ChEMBL 179 1 0 4 0.8 Cc1noc(C2CN3CCC2C3)n1 10.1021/jm00083a016
CHEMBL1223754 15714 0 None -50 5 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
9820835 116053 2 None - 1 Human 5.7 pEC50 = 5.7 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 179 2 1 5 0.1 CCn1nnc(C2=CCCNC2)n1 10.1021/jm00050a006
CHEMBL337676 116053 2 None - 1 Human 5.7 pEC50 = 5.7 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 179 2 1 5 0.1 CCn1nnc(C2=CCCNC2)n1 10.1021/jm00050a006
9927975 3962 0 None -10 2 Human 8.7 pEC50 = 8.7 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 341 3 0 5 3.5 C(#Cc1ccccc1)CSc1nsnc1[C@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL100147 3962 0 None -10 2 Human 8.7 pEC50 = 8.7 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 341 3 0 5 3.5 C(#Cc1ccccc1)CSc1nsnc1[C@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
145973726 163827 0 None -36 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M2 receptor assessed as increase in acetylcholine-induced responsePositive allosteric modulation of human M2 receptor assessed as increase in acetylcholine-induced response
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216213 163827 0 None -36 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human M2 receptor assessed as increase in acetylcholine-induced responsePositive allosteric modulation of human M2 receptor assessed as increase in acetylcholine-induced response
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
137629935 160217 0 None -1 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 160217 0 None -1 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 160217 0 None -1 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
122191003 122860 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 509 6 3 3 4.9 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618446 122860 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 509 6 3 3 4.9 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
137635723 155296 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Activity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilizationActivity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 9 2.5 Cc1nnc2sc(C(=O)NC3CN(c4nc5cccnc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4062934 155296 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Activity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilizationActivity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 9 2.5 Cc1nnc2sc(C(=O)NC3CN(c4nc5cccnc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
187 246 29 None -2 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M2 receptor expressed in CHO-K1 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
294 246 29 None -2 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M2 receptor expressed in CHO-K1 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
65 246 29 None -2 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M2 receptor expressed in CHO-K1 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 246 29 None -2 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M2 receptor expressed in CHO-K1 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 246 29 None -2 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M2 receptor expressed in CHO-K1 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 246 29 None -2 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M2 receptor expressed in CHO-K1 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
187 246 29 None -2 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
294 246 29 None -2 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
65 246 29 None -2 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
8593 246 29 None -2 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
CHEMBL667 246 29 None -2 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
DB03128 246 29 None -2 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
137630667 160289 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 204 3 0 1 2.7 C[N+](C)(C)CCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
CHEMBL4100938 160289 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 204 3 0 1 2.7 C[N+](C)(C)CCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116890 160289 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 204 3 0 1 2.7 C[N+](C)(C)CCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
57230548 172413 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC[C@@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL4524085 172413 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC[C@@H]1C2 10.1016/s0960-894x(98)00509-5
44330080 107020 0 None -8 2 Human 6.6 pEC50 = 6.6 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL319109 107020 0 None -8 2 Human 6.6 pEC50 = 6.6 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
44303018 197602 0 None -218 3 Human 5.6 pEC50 = 5.6 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 343 3 0 5 2.4 Clc1cccc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL60833 197602 0 None -218 3 Human 5.6 pEC50 = 5.6 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 343 3 0 5 2.4 Clc1cccc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
137631026 160347 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 230 1 0 1 3.0 C[N+](C)(C)C1CCc2ccc3ccoc3c2C1 10.1021/acs.jmedchem.7b01113
CHEMBL4093215 160347 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 230 1 0 1 3.0 C[N+](C)(C)C1CCc2ccc3ccoc3c2C1 10.1021/acs.jmedchem.7b01113
CHEMBL4117321 160347 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 230 1 0 1 3.0 C[N+](C)(C)C1CCc2ccc3ccoc3c2C1 10.1021/acs.jmedchem.7b01113
137628799 160190 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 160190 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 160190 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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
CHEMBL3616504 122585 0 None 3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 441 3 2 3 4.0 CN1CCCC/C1=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2 10.1016/j.bmcl.2015.08.011
10686494 99861 0 None -16 3 Human 6.6 pEC50 = 6.6 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1 10.1016/s0960-894x(98)00509-5
CHEMBL291351 99861 0 None -16 3 Human 6.6 pEC50 = 6.6 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1 10.1016/s0960-894x(98)00509-5
10686494 99861 0 None -16 3 Human 6.6 pEC50 = 6.6 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1 10.1021/jm9910019
CHEMBL291351 99861 0 None -16 3 Human 6.6 pEC50 = 6.6 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1 10.1021/jm9910019
CHEMBL3618449 122863 0 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 449 5 2 3 4.5 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL1223863 15764 0 None -794 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223864 15765 0 None -199 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223941 15785 0 None -251 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
89777060 156329 0 None -114 2 Human 5.6 pEC50 = 5.6 Functional
Activity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilizationActivity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 3 2 7 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Oc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4074908 156329 0 None -114 2 Human 5.6 pEC50 = 5.6 Functional
Activity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilizationActivity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 3 2 7 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Oc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
5487543 201197 1 None -223 3 Human 4.6 pEC50 = 4.6 Functional
Compound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm9910019
CHEMBL81878 201197 1 None -223 3 Human 4.6 pEC50 = 4.6 Functional
Compound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm9910019
11725107 99936 0 None -134 3 Human 5.6 pEC50 = 5.6 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 345 3 0 5 2.1 Fc1cc(F)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL291872 99936 0 None -134 3 Human 5.6 pEC50 = 5.6 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 345 3 0 5 2.1 Fc1cc(F)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
137629887 160207 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 218 4 0 1 3.1 C[N+](C)(C)CCCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
CHEMBL4065555 160207 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 218 4 0 1 3.1 C[N+](C)(C)CCCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
CHEMBL4116259 160207 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 218 4 0 1 3.1 C[N+](C)(C)CCCc1ccc2ccoc2c1 10.1021/acs.jmedchem.7b01113
10375002 23774 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 178 2 1 4 0.7 CCn1ncc(C2=CCCNC2)n1 10.1021/jm00050a006
CHEMBL133905 23774 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 178 2 1 4 0.7 CCn1ncc(C2=CCCNC2)n1 10.1021/jm00050a006
44158142 187829 34 None -1 4 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat muscarinic M2 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at rat muscarinic M2 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 187829 34 None -1 4 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat muscarinic M2 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at rat muscarinic M2 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
5487543 201197 1 None -223 3 Human 4.6 pEC50 = 4.6 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1016/s0960-894x(98)00509-5
CHEMBL81878 201197 1 None -223 3 Human 4.6 pEC50 = 4.6 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1016/s0960-894x(98)00509-5
650899 53944 10 None -10 5 Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1535797 53944 10 None -10 5 Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1609153 53944 10 None -10 5 Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
44158142 187829 34 None -1 4 Rat 5.6 pEC50 = 5.6 Functional
Activation of rat muscarinic M2 receptor expressed in CHO cells co-expressing chimeric Gqi5 protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of rat muscarinic M2 receptor expressed in CHO cells co-expressing chimeric Gqi5 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 187829 34 None -1 4 Rat 5.6 pEC50 = 5.6 Functional
Activation of rat muscarinic M2 receptor expressed in CHO cells co-expressing chimeric Gqi5 protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of rat muscarinic M2 receptor expressed in CHO cells co-expressing chimeric Gqi5 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
57088082 172414 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@@H]1CN2CCC[C@@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL4524086 172414 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@@H]1CN2CCC[C@@H]1C2 10.1016/s0960-894x(98)00509-5
53414666 158498 7 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 192 4 1 3 1.2 c1cncc(COCC2CCNC2)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4099673 158498 7 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 192 4 1 3 1.2 c1cncc(COCC2CCNC2)c1 10.1021/acs.jmedchem.7b01113
178030 21003 24 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 5 0.4 CCn1nnc(C2=CCCN(C)C2)n1 10.1016/j.bmcl.2015.08.011
CHEMBL131428 21003 24 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 5 0.4 CCn1nnc(C2=CCCN(C)C2)n1 10.1016/j.bmcl.2015.08.011
129456 202706 11 None 8 2 Human 8.5 pEC50 = 8.5 Functional
In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by Muscarinic M2 receptor)In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by Muscarinic M2 receptor)
ChEMBL 179 1 0 4 0.8 Cc1noc(C2CN3CCC2C3)n1 10.1021/jm00083a016
CHEMBL92421 202706 11 None 8 2 Human 8.5 pEC50 = 8.5 Functional
In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by Muscarinic M2 receptor)In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by Muscarinic M2 receptor)
ChEMBL 179 1 0 4 0.8 Cc1noc(C2CN3CCC2C3)n1 10.1021/jm00083a016
137629935 160217 0 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 160217 0 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 160217 0 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
137629935 160217 0 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 160217 0 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 160217 0 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting method
ChEMBL 206 3 0 1 1.9 C[N+](C)(C)CCc1ccc2c(c1)OCC2 10.1021/acs.jmedchem.7b01113
CHEMBL3618448 122862 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 523 6 2 3 5.2 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)N(C)CCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
3652 3869 67 None -18 9 Human 6.4 pEC50 = 6.4 Functional
Compound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
57 3869 67 None -18 9 Human 6.4 pEC50 = 6.4 Functional
Compound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
60809 3869 67 None -18 9 Human 6.4 pEC50 = 6.4 Functional
Compound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
CHEMBL21536 3869 67 None -18 9 Human 6.4 pEC50 = 6.4 Functional
Compound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
DB15357 3869 67 None -18 9 Human 6.4 pEC50 = 6.4 Functional
Compound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
CHEMBL1223862 15763 0 None -158 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
87934 97419 20 None - 1 Human 6.4 pEC50 = 6.4 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 210 1 0 3 0.5 CCN1C(=O)CC2(CCN(C)CC2)C1=O 10.1021/jm00050a006
CHEMBL273308 97419 20 None - 1 Human 6.4 pEC50 = 6.4 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 210 1 0 3 0.5 CCN1C(=O)CC2(CCN(C)CC2)C1=O 10.1021/jm00050a006
CHEMBL542883 97419 20 None - 1 Human 6.4 pEC50 = 6.4 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 210 1 0 3 0.5 CCN1C(=O)CC2(CCN(C)CC2)C1=O 10.1021/jm00050a006
122191004 122580 0 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 521 7 3 4 4.7 COc1ccc(CCN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3616497 122580 0 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 521 7 3 4 4.7 COc1ccc(CCN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
122191001 122858 0 None -9 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1cccc(F)c1 10.1016/j.bmcl.2015.08.011
CHEMBL3618444 122858 0 None -9 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1cccc(F)c1 10.1016/j.bmcl.2015.08.011
187 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
647412 26944 9 None -3 4 Human 4.3 pEC50 = 4.3 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
CHEMBL1367424 26944 9 None -3 4 Human 4.3 pEC50 = 4.3 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
187 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
8593 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL667 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
DB03128 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
137639541 155913 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 206 3 0 3 1.7 CN1CCCC(OCc2cccnc2)C1 10.1021/acs.jmedchem.7b01113
CHEMBL4070061 155913 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 206 3 0 3 1.7 CN1CCCC(OCc2cccnc2)C1 10.1021/acs.jmedchem.7b01113
CHEMBL1223860 15761 0 None -501 5 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
187 246 29 None -2 6 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 246 29 None -2 6 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 246 29 None -2 6 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 246 29 None -2 6 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 246 29 None -2 6 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 246 29 None -2 6 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
187 246 29 None -2 6 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 246 29 None -2 6 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 246 29 None -2 6 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 246 29 None -2 6 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 246 29 None -2 6 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 246 29 None -2 6 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
44303293 197004 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 393 3 0 5 3.8 Clc1cc(Cl)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL60479 197004 0 None 1 3 Human 6.3 pEC50 = 6.3 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 393 3 0 5 3.8 Clc1cc(Cl)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
53382542 85675 0 None -7 6 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M2 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M2 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313377 85675 0 None -7 6 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human muscarinic M2 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M2 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
187 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
294 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
65 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 246 29 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL3618447 122861 0 None -3 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 509 5 2 3 5.2 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
2551 755 22 None -2 12 Human 4.2 pEC50 = 4.2 Functional
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M2Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M2
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
298 755 22 None -2 12 Human 4.2 pEC50 = 4.2 Functional
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M2Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M2
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
488 755 22 None -2 12 Human 4.2 pEC50 = 4.2 Functional
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M2Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M2
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
CHEMBL965 755 22 None -2 12 Human 4.2 pEC50 = 4.2 Functional
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M2Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M2
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
DB00411 755 22 None -2 12 Human 4.2 pEC50 = 4.2 Functional
Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M2Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M2
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
10426487 2686 3 None -3 2 Human 7.2 pEC50 = 7.2 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 10.1016/s0960-894x(98)00509-5
291 2686 3 None -3 2 Human 7.2 pEC50 = 7.2 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 10.1016/s0960-894x(98)00509-5
CHEMBL99521 2686 3 None -3 2 Human 7.2 pEC50 = 7.2 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 10.1016/s0960-894x(98)00509-5
306 3259 15 None -1 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 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 3259 15 None -1 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 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 3259 15 None -1 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 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 3259 15 None -1 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 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 3259 15 None -1 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 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
CHEMBL1223803 15736 0 None -125 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223805 15738 0 None -199 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223940 15784 0 None -251 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
16071018 15713 14 None -112 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
CHEMBL1223753 15713 14 None -112 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
16038385 79840 0 None -10 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 301 2 1 4 2.1 O=c1[nH]c2ccccc2n1C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
CHEMBL2146598 79840 0 None -10 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 301 2 1 4 2.1 O=c1[nH]c2ccccc2n1C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
16123945 79841 8 None -125 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
CHEMBL2146599 79841 8 None -125 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
170332 160173 1 None -2 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4091934 160173 1 None -2 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115997 160173 1 None -2 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
2166 2946 43 None -95 8 Human 4.2 pEC50 = 4.2 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/s0960-894x(98)00509-5
305 2946 43 None -95 8 Human 4.2 pEC50 = 4.2 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/s0960-894x(98)00509-5
5910 2946 43 None -95 8 Human 4.2 pEC50 = 4.2 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/s0960-894x(98)00509-5
CHEMBL550 2946 43 None -95 8 Human 4.2 pEC50 = 4.2 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/s0960-894x(98)00509-5
DB01085 2946 43 None -95 8 Human 4.2 pEC50 = 4.2 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/s0960-894x(98)00509-5
170332 160173 1 None -2 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4091934 160173 1 None -2 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4115997 160173 1 None -2 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assayAgonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by FRET assay
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
CHEMBL3616499 122582 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 445 5 2 3 4.7 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618450 122864 0 None -2 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 465 5 2 3 5.0 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Cl)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
44303397 101607 0 None -75 3 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 359 3 0 5 3.1 Clc1cccc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL303360 101607 0 None -75 3 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 359 3 0 5 3.1 Clc1cccc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
10104047 21269 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 192 3 1 4 0.9 C=CCn1ncc(C2CCCNC2)n1 10.1021/jm00050a006
CHEMBL131777 21269 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 192 3 1 4 0.9 C=CCn1ncc(C2CCCNC2)n1 10.1021/jm00050a006
10019339 101940 0 None -138 3 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 327 3 0 5 1.9 Fc1cccc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL304247 101940 0 None -138 3 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 327 3 0 5 1.9 Fc1cccc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL3616501 122584 0 None -30 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 2 3 6.1 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(-c3ccccc3)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
187 246 29 None -2 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 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
294 246 29 None -2 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 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
65 246 29 None -2 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 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 246 29 None -2 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 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 246 29 None -2 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 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 246 29 None -2 6 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 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 755 22 None -2 12 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9910019
298 755 22 None -2 12 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9910019
488 755 22 None -2 12 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9910019
CHEMBL965 755 22 None -2 12 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9910019
DB00411 755 22 None -2 12 Human 6.2 pEC50 = 6.2 Functional
Compound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency towards Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9910019
2551 755 22 None -2 12 Human 6.2 pEC50 = 6.2 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00509-5
298 755 22 None -2 12 Human 6.2 pEC50 = 6.2 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00509-5
488 755 22 None -2 12 Human 6.2 pEC50 = 6.2 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00509-5
CHEMBL965 755 22 None -2 12 Human 6.2 pEC50 = 6.2 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00509-5
DB00411 755 22 None -2 12 Human 6.2 pEC50 = 6.2 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00509-5
59654579 122854 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618440 122854 0 None -3 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
122190994 122851 0 None -14 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 481 4 3 3 5.1 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)Nc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618436 122851 0 None -14 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 481 4 3 3 5.1 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)Nc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
44303294 196734 0 None -16 3 Human 6.1 pEC50 = 6.1 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 377 3 0 5 3.3 Fc1cc(Cl)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL60331 196734 0 None -16 3 Human 6.1 pEC50 = 6.1 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 377 3 0 5 3.3 Fc1cc(Cl)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
170332 160173 1 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 160173 1 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 160173 1 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
44303286 196896 0 None -48 3 Human 6.1 pEC50 = 6.1 Functional
Compound was tested for its potency at Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency at Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 309 3 0 5 1.8 C(#Cc1ccccc1)COc1nsnc1C12CN3CC1C2C3 10.1021/jm9910019
CHEMBL60419 196896 0 None -48 3 Human 6.1 pEC50 = 6.1 Functional
Compound was tested for its potency at Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cellsCompound was tested for its potency at Muscarinic acetylcholine receptor M2 by inhibiting forskolin induced c-AMP formation in CHO-M2 cells
ChEMBL 309 3 0 5 1.8 C(#Cc1ccccc1)COc1nsnc1C12CN3CC1C2C3 10.1021/jm9910019
44303286 196896 0 None -48 3 Human 6.1 pEC50 = 6.1 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 309 3 0 5 1.8 C(#Cc1ccccc1)COc1nsnc1C12CN3CC1C2C3 10.1016/s0960-894x(98)00509-5
CHEMBL60419 196896 0 None -48 3 Human 6.1 pEC50 = 6.1 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 309 3 0 5 1.8 C(#Cc1ccccc1)COc1nsnc1C12CN3CC1C2C3 10.1016/s0960-894x(98)00509-5
170332 160173 1 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 160173 1 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins 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 160173 1 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting methodAgonist activity at Gi/o protein-coupled recombinant human muscarinic M2 receptor expressed in CHO-FlpIn cells preincubated for 60 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1cccc(CC[N+](C)(C)C)c1 10.1021/acs.jmedchem.7b01113
44253016 79839 2 None -6 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
CHEMBL2146597 79839 2 None -6 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
44303019 100267 0 None -79 3 Human 6.1 pEC50 = 6.1 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 327 3 0 5 1.9 Fc1ccc(C#CCOc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
CHEMBL294082 100267 0 None -79 3 Human 6.1 pEC50 = 6.1 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 327 3 0 5 1.9 Fc1ccc(C#CCOc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
16071018 15713 14 None -112 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223753 15713 14 None -112 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223861 15762 0 None -630 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223939 15783 0 None -316 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
9883040 99860 0 None -7 3 Human 8.1 pEC50 = 8.1 Functional
In vitro functional agonism against M2 muscarinic receptor (cAMP)In vitro functional agonism against M2 muscarinic receptor (cAMP)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL291339 99860 0 None -7 3 Human 8.1 pEC50 = 8.1 Functional
In vitro functional agonism against M2 muscarinic receptor (cAMP)In vitro functional agonism against M2 muscarinic receptor (cAMP)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL542622 99860 0 None -7 3 Human 8.1 pEC50 = 8.1 Functional
In vitro functional agonism against M2 muscarinic receptor (cAMP)In vitro functional agonism against M2 muscarinic receptor (cAMP)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
44303396 196814 0 None 1 3 Human 7.1 pEC50 = 7.1 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 359 3 0 5 3.1 Clc1ccc(C#CCSc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
CHEMBL60374 196814 0 None 1 3 Human 7.1 pEC50 = 7.1 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 359 3 0 5 3.1 Clc1ccc(C#CCSc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
118500 156207 55 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 165 4 1 2 1.5 CNCCc1cccc(OC)c1 10.1021/acs.jmedchem.7b01113
CHEMBL4073256 156207 55 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 165 4 1 2 1.5 CNCCc1cccc(OC)c1 10.1021/acs.jmedchem.7b01113
44303323 162438 0 None -18 3 Human 7.1 pEC50 = 7.1 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 343 3 0 5 2.6 Fc1ccc(C#CCSc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
CHEMBL418491 162438 0 None -18 3 Human 7.1 pEC50 = 7.1 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 343 3 0 5 2.6 Fc1ccc(C#CCSc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
10104047 21269 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 192 3 1 4 0.9 C=CCn1ncc(C2CCCNC2)n1 10.1021/jm00050a006
CHEMBL131777 21269 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
M2 agonist activity estimated by depression of isolated guinea pig left atriumM2 agonist activity estimated by depression of isolated guinea pig left atrium
ChEMBL 192 3 1 4 0.9 C=CCn1ncc(C2CCCNC2)n1 10.1021/jm00050a006
71792 77787 27 None -2 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 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 77787 27 None -2 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M2 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
44303327 162208 0 None -31 3 Human 6.1 pEC50 = 6.1 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 325 3 0 5 2.5 C(#Cc1ccccc1)CSc1nsnc1C12CN3CC1C2C3 10.1021/jm9910019
CHEMBL417560 162208 0 None -31 3 Human 6.1 pEC50 = 6.1 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 325 3 0 5 2.5 C(#Cc1ccccc1)CSc1nsnc1C12CN3CC1C2C3 10.1021/jm9910019
2551 755 22 None -2 12 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
298 755 22 None -2 12 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
488 755 22 None -2 12 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 755 22 None -2 12 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol 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 755 22 None -2 12 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
44330081 203686 0 None -17 2 Human 8.1 pEC50 = 8.1 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL98255 203686 0 None -17 2 Human 8.1 pEC50 = 8.1 Functional
Stimulation of cAMP in CHO cells expressing human m2 receptorStimulation of cAMP in CHO cells expressing human m2 receptor
ChEMBL 325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
44303314 100254 0 None -363 3 Human 6.0 pEC50 = 6.0 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 343 3 0 5 2.6 Fc1cccc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL293982 100254 0 None -363 3 Human 6.0 pEC50 = 6.0 Functional
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptorCompound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
ChEMBL 343 3 0 5 2.6 Fc1cccc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
137629744 160372 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1ccccc1CC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL4071109 160372 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1ccccc1CC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
CHEMBL4117602 160372 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 194 4 0 1 1.9 COc1ccccc1CC[N+](C)(C)C 10.1021/acs.jmedchem.7b01113
644390 40000 6 None -3 4 Human 4.0 pEC50 = 4.0 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
CHEMBL1482157 40000 6 None -3 4 Human 4.0 pEC50 = 4.0 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
25010776 55476 1 None -44 5 Human 4.0 pEC50 = 4.0 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 nan
CHEMBL1559151 55476 1 None -44 5 Human 4.0 pEC50 = 4.0 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 nan
CHEMBL1624037 55476 1 None -44 5 Human 4.0 pEC50 = 4.0 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M2. (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen), 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay)]
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 nan
137646732 156996 0 None -12 2 Human 6.0 pEC50 = 6.0 Functional
Activity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilizationActivity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 422 3 2 7 2.9 Cc1nnc2sc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4083081 156996 0 None -12 2 Human 6.0 pEC50 = 6.0 Functional
Activity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilizationActivity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 422 3 2 7 2.9 Cc1nnc2sc(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
75356563 156165 17 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 184 3 1 4 1.0 c1csc(COC2CCNC2)n1 10.1021/acs.jmedchem.7b01113
CHEMBL4072787 156165 17 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting methodAgonist activity at human recombinant muscarinic M2 receptor co-expressed with Galphaqi5-HA in African green monkey COS7 cells assessed as IP accumulation after 2 hrs in presence of myo-[3H]inositol by liquid scintillation counting method
ChEMBL 184 3 1 4 1.0 c1csc(COC2CCNC2)n1 10.1021/acs.jmedchem.7b01113
9913341 81538 2 None 28 3 Human 9.3 pIC50 = 9.3 Functional
Activity at human M2 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M2 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL216927 81538 2 None 28 3 Human 9.3 pIC50 = 9.3 Functional
Activity at human M2 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M2 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL553058 81538 2 None 28 3 Human 9.3 pIC50 = 9.3 Functional
Activity at human M2 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M2 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
44590172 169502 0 None 1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 169502 0 None 1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 169502 0 None 1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 177916 0 None 1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 177916 0 None 1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 177916 0 None 1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
44590176 188219 0 None 3 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 188219 0 None 3 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 188219 0 None 3 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
155566290 175756 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation pre-incubated for 30 mins followed by carbachol addition and measured after 1 hr by HTRF assayAntagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation pre-incubated for 30 mins followed by carbachol addition and measured after 1 hr by HTRF assay
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 175756 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation pre-incubated for 30 mins followed by carbachol addition and measured after 1 hr by HTRF assayAntagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation pre-incubated for 30 mins followed by carbachol addition and measured after 1 hr by HTRF assay
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 175756 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation pre-incubated for 30 mins followed by carbachol addition and measured after 1 hr by HTRF assayAntagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation pre-incubated for 30 mins followed by carbachol addition and measured after 1 hr by HTRF assay
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
CHEMBL3085072 105806 0 None -5 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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 105806 0 None -5 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
44590179 171898 0 None 1 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 171898 0 None 1 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 171898 0 None 1 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
44590167 178187 0 None -3 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 178187 0 None -3 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
44589495 185143 0 None -10 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 185143 0 None -10 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
44590122 189548 0 None -15 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 189548 0 None -15 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
16125400 84029 0 None - 1 Human 6.0 pIC50 = 6 Functional
Activity at muscarinic M2 receptor in Albino Dunkin-Hartley guinea pig left atria assessed as inhibition of methacholine-induced bradycardiaActivity at muscarinic M2 receptor in Albino Dunkin-Hartley guinea pig left atria assessed as inhibition of methacholine-induced bradycardia
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 84029 0 None - 1 Human 6.0 pIC50 = 6 Functional
Activity at muscarinic M2 receptor in Albino Dunkin-Hartley guinea pig left atria assessed as inhibition of methacholine-induced bradycardiaActivity at muscarinic M2 receptor in Albino Dunkin-Hartley guinea pig left atria assessed as inhibition of methacholine-induced bradycardia
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+
CHEMBL3085066 105814 0 None -1 3 Human 6.0 pIC50 = 6 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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 105814 0 None -1 3 Human 6.0 pIC50 = 6 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
CHEMBL4796491 182421 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 300 5 1 3 3.2 O=C(CCN1CCCc2ccccc21)NCc1cccs1 10.1016/j.bmcl.2020.127632
71455968 83301 0 None -2 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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 83301 0 None -2 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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
10397133 106366 1 None 1 3 Human 6.0 pIC50 = 6.0 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 164 2 0 3 0.3 C#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL315676 106366 1 None 1 3 Human 6.0 pIC50 = 6.0 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 164 2 0 3 0.3 C#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
71716773 85928 0 None 2 2 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 428 4 1 5 2.9 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccc(C(F)(F)F)nc3)C2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL2315680 85928 0 None 2 2 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 428 4 1 5 2.9 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccc(C(F)(F)F)nc3)C2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL4763422 180548 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 302 4 1 3 2.2 O=C(CCN1CCCc2ccccc21)N1CCCCC1CO 10.1016/j.bmcl.2020.127632
71463135 83309 0 None -2 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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 83309 0 None -2 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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
71716773 85928 0 None 2 2 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 428 4 1 5 2.9 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccc(C(F)(F)F)nc3)C2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL2315680 85928 0 None 2 2 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
ChEMBL 428 4 1 5 2.9 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccc(C(F)(F)F)nc3)C2)CC1 10.1016/j.bmcl.2012.10.132
109018479 180979 1 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 284 5 1 3 2.7 O=C(CCN1CCCc2ccccc21)NCc1ccco1 10.1016/j.bmcl.2020.127632
CHEMBL4778178 180979 1 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 284 5 1 3 2.7 O=C(CCN1CCCc2ccccc21)NCc1ccco1 10.1016/j.bmcl.2020.127632
CHEMBL3085084 102807 0 None 1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
CHEMBL3084639 102690 0 None -11 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human cloned muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M2 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
CHEMBL3085059 105811 0 None -5 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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 105811 0 None -5 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
44590180 171827 0 None 1 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 171827 0 None 1 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 171827 0 None 1 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
44590175 187791 0 None 3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 187791 0 None 3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 187791 0 None 3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
52176747 158229 1 None -2 8 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M2 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 158229 1 None -2 8 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M2 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
CHEMBL4758449 180124 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 244 3 0 2 2.1 O=C(CCN1CCCc2ccccc21)N1CCC1 10.1016/j.bmcl.2020.127632
25034111 190078 0 None -7 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 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 190078 0 None -7 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 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
44590123 183023 0 None -15 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 183023 0 None -15 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
25034111 190078 0 None -7 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 190078 0 None -7 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
44589497 174473 0 None -5 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 174473 0 None -5 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
CHEMBL2307674 85408 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human cloned muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M2 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
10092649 189733 47 None -16 11 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M2 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 189733 47 None -16 11 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M2 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 189733 47 None -16 11 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M2 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 189733 47 None -16 11 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M2 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
290 2338 2 None -21 5 Human 4.9 pIC50 = 4.9 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/S0960-894X(00)80538-7
4022 2338 2 None -21 5 Human 4.9 pIC50 = 4.9 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/S0960-894X(00)80538-7
5926 2338 2 None -21 5 Human 4.9 pIC50 = 4.9 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/S0960-894X(00)80538-7
CHEMBL40554 2338 2 None -21 5 Human 4.9 pIC50 = 4.9 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/S0960-894X(00)80538-7
CHEMBL74300 2338 2 None -21 5 Human 4.9 pIC50 = 4.9 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/S0960-894X(00)80538-7
71450616 83308 0 None -2 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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 83308 0 None -2 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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
CHEMBL3085071 105819 0 None -5 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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 105819 0 None -5 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
CHEMBL3085083 102806 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
CHEMBL3085080 102803 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
13940563 201576 5 None 5 2 Rat 5.9 pIC50 = 5.9 Functional
Muscarinic receptor M2 in rat heart using [3H]QNB (quinuclidinyl benzylate) radioligand as a M2 non-selective muscarinic receptor antagonist at a concentration of 0.12 nMMuscarinic receptor M2 in rat heart using [3H]QNB (quinuclidinyl benzylate) radioligand as a M2 non-selective muscarinic receptor antagonist at a concentration of 0.12 nM
ChEMBL 182 2 0 3 -0.3 CN(C)CC#CCN1OCCC1=O 10.1016/S0960-894X(97)00150-9
CHEMBL8510 201576 5 None 5 2 Rat 5.9 pIC50 = 5.9 Functional
Muscarinic receptor M2 in rat heart using [3H]QNB (quinuclidinyl benzylate) radioligand as a M2 non-selective muscarinic receptor antagonist at a concentration of 0.12 nMMuscarinic receptor M2 in rat heart using [3H]QNB (quinuclidinyl benzylate) radioligand as a M2 non-selective muscarinic receptor antagonist at a concentration of 0.12 nM
ChEMBL 182 2 0 3 -0.3 CN(C)CC#CCN1OCCC1=O 10.1016/S0960-894X(97)00150-9
CHEMBL4740422 178601 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 312 5 1 2 3.3 O=C(CCN1CCCc2ccccc21)NCc1cccc(F)c1 10.1016/j.bmcl.2020.127632
16664965 84267 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at muscarinic M2 receptor in Albino Dunkin-Hartley guinea pig left atria assessed as inhibition of methacholine-induced bradycardiaActivity at muscarinic M2 receptor in Albino Dunkin-Hartley guinea pig left atria assessed as inhibition of methacholine-induced bradycardia
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 84267 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at muscarinic M2 receptor in Albino Dunkin-Hartley guinea pig left atria assessed as inhibition of methacholine-induced bradycardiaActivity at muscarinic M2 receptor in Albino Dunkin-Hartley guinea pig left atria assessed as inhibition of methacholine-induced bradycardia
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+
CHEMBL3085082 102805 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
109035013 179637 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 314 4 1 2 4.1 O=C(CCN1CCCc2ccccc21)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2020.127632
CHEMBL4752973 179637 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 314 4 1 2 4.1 O=C(CCN1CCCc2ccccc21)Nc1ccc(Cl)cc1 10.1016/j.bmcl.2020.127632
CHEMBL3085079 102801 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
CHEMBL3085065 105813 0 None -5 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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 105813 0 None -5 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
71459691 83307 0 None 5 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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 83307 0 None 5 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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
44590170 187532 0 None 1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 187532 0 None 1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 187532 0 None 1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
109032820 182038 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 286 3 0 2 3.1 CC1CCCN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
CHEMBL4791819 182038 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 286 3 0 2 3.1 CC1CCCN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
CHEMBL4756442 179957 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC(O)CC1 10.1016/j.bmcl.2020.127632
CHEMBL3084663 102703 0 None -1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human cloned muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M2 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
15681301 119579 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 178 3 0 3 0.7 C#CCCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL352832 119579 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 178 3 0 3 0.7 C#CCCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
15945874 187923 0 None -7 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 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 187923 0 None -7 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 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
15945874 187923 0 None -7 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 187923 0 None -7 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 189125 0 None -7 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 189125 0 None -7 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
44590035 189357 0 None -3 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 189357 0 None -3 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
25034180 187573 0 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 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 187573 0 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 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
44589571 171769 0 None -10 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 171769 0 None -10 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
44589570 171939 0 None -15 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 171939 0 None -15 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
10465524 58497 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 204 3 0 3 1.3 C=CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL169011 58497 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 204 3 0 3 1.3 C=CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
137630050 160237 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Competitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 0.1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF assayCompetitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 0.1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF 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 160237 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Competitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 0.1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF assayCompetitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 0.1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF 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 160237 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Competitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 0.1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF assayCompetitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 0.1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF 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 160237 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Competitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 0.1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF assayCompetitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 0.1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF 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
15681299 119739 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 180 2 0 3 1.2 C1CC(O/N=C2\CN3CCC2C3)C1 10.1016/S0960-894X(00)80538-7
CHEMBL354259 119739 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 180 2 0 3 1.2 C1CC(O/N=C2\CN3CCC2C3)C1 10.1016/S0960-894X(00)80538-7
156015978 177499 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4636899 177499 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651111 177499 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assayAntagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 22 degree C pre-incubated for 180 mins followed by carbachol addition and further incubated at 37 degree C for 90 mins by HTRF assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
10397356 119971 0 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL354738 119971 0 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
137630050 160237 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Competitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF assayCompetitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF 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 160237 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Competitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF assayCompetitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF 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 160237 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Competitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF assayCompetitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF 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 160237 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Competitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF assayCompetitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 1 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF 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
CHEMBL4758633 180141 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCC[C@H]1CO 10.1016/j.bmcl.2020.127632
71459689 83291 0 None 1 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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 83291 0 None 1 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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
71454215 83300 0 None -3 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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 83300 0 None -3 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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
109013312 179297 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 258 3 0 2 2.5 O=C(CCN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4748774 179297 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 258 3 0 2 2.5 O=C(CCN1CCCc2ccccc21)N1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4759774 180233 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 393 2 0 5 4.0 CC(C)(C)OC(=O)N1CCN(CC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.bmcl.2020.127632
CHEMBL3085091 102814 0 None -2 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
CHEMBL3085086 102809 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
CHEMBL4760037 180252 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 288 4 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC1CO 10.1016/j.bmcl.2020.127632
71452455 83294 0 None -3 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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 83294 0 None -3 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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
44590125 183024 0 None -12 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 183024 0 None -12 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
44590036 187538 0 None -6 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 187538 0 None -6 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
152278786 181915 0 None -117 4 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic receptor M2 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M2 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 181915 0 None -117 4 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic receptor M2 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M2 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
CHEMBL4742997 178802 0 None -154 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant muscarinic receptor M2 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M2 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
25034112 187554 0 None -1 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 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 187554 0 None -1 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 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
44589585 188048 0 None -1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 188048 0 None -1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 188048 0 None -1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
44590177 188078 0 None 3 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 188078 0 None 3 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 188078 0 None 3 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
163938 106222 12 None 316 2 Human 7.7 pIC50 = 7.7 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 180 1 1 5 0.1 Nc1noc(C2CN3CCC2C3)n1 10.1016/S0960-894X(00)80538-7
CHEMBL314737 106222 12 None 316 2 Human 7.7 pIC50 = 7.7 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 180 1 1 5 0.1 Nc1noc(C2CN3CCC2C3)n1 10.1016/S0960-894X(00)80538-7
152278786 181915 0 None -117 4 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic receptor M2 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M2 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 181915 0 None -117 4 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic receptor M2 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M2 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
CHEMBL4745885 179057 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 274 4 0 3 1.7 COC1CN(C(=O)CCN2CCCc3ccccc32)C1 10.1016/j.bmcl.2020.127632
10262405 57103 0 None -2 2 Human 4.7 pIC50 = 4.7 Functional
Compound was evaluated for inhibitory activity for Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsCompound was evaluated for inhibitory activity for Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 206 3 0 3 1.5 CCCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL166782 57103 0 None -2 2 Human 4.7 pIC50 = 4.7 Functional
Compound was evaluated for inhibitory activity for Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsCompound was evaluated for inhibitory activity for Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 206 3 0 3 1.5 CCCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL3084670 102708 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human cloned muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M2 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
10262466 97680 0 None -10 2 Rat 6.7 pIC50 = 6.7 Functional
Muscarinic receptor M2 in rat heart using [3H]QNB (quinuclidinyl benzylate) radioligand as a M2 non-selective muscarinic receptor antagonist at a concentration of 0.12 nMMuscarinic receptor M2 in rat heart using [3H]QNB (quinuclidinyl benzylate) radioligand as a M2 non-selective muscarinic receptor antagonist at a concentration of 0.12 nM
ChEMBL 208 2 0 3 0.3 O=C1CCON1CC#CCN1CCCC1 10.1016/S0960-894X(97)00150-9
CHEMBL275104 97680 0 None -10 2 Rat 6.7 pIC50 = 6.7 Functional
Muscarinic receptor M2 in rat heart using [3H]QNB (quinuclidinyl benzylate) radioligand as a M2 non-selective muscarinic receptor antagonist at a concentration of 0.12 nMMuscarinic receptor M2 in rat heart using [3H]QNB (quinuclidinyl benzylate) radioligand as a M2 non-selective muscarinic receptor antagonist at a concentration of 0.12 nM
ChEMBL 208 2 0 3 0.3 O=C1CCON1CC#CCN1CCCC1 10.1016/S0960-894X(97)00150-9
CHEMBL3085081 102804 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
10399393 201336 0 None 1 2 Human 5.7 pIC50 = 5.7 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 240 2 0 3 1.1 C#CCC#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL83074 201336 0 None 1 2 Human 5.7 pIC50 = 5.7 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 240 2 0 3 1.1 C#CCC#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL4760150 180263 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 300 3 0 2 3.6 CC1CCCC(C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
156015807 177475 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 37 degree C pre-incubated for 30 mins followed by carbachol addition and measured after 60 mins by HTRF assayAntagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 37 degree C pre-incubated for 30 mins followed by carbachol addition and measured after 60 mins by HTRF assay
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4641726 177475 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 37 degree C pre-incubated for 30 mins followed by carbachol addition and measured after 60 mins by HTRF assayAntagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 37 degree C pre-incubated for 30 mins followed by carbachol addition and measured after 60 mins by HTRF assay
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4650973 177475 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 37 degree C pre-incubated for 30 mins followed by carbachol addition and measured after 60 mins by HTRF assayAntagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 37 degree C pre-incubated for 30 mins followed by carbachol addition and measured after 60 mins by HTRF assay
ChEMBL 1185 25 3 12 9.5 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCCN3CCN(CCCCC4CCN(CC(=O)N5c6ccccc6NC(=O)c6ccccc65)CC4)CC3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL3085070 105782 0 None -15 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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 105782 0 None -15 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
156015978 177499 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 37 degree C pre-incubated for 30 mins followed by carbachol addition and measured after 60 mins by HTRF assayAntagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 37 degree C pre-incubated for 30 mins followed by carbachol addition and measured after 60 mins by HTRF assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4636899 177499 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 37 degree C pre-incubated for 30 mins followed by carbachol addition and measured after 60 mins by HTRF assayAntagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 37 degree C pre-incubated for 30 mins followed by carbachol addition and measured after 60 mins by HTRF assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4651111 177499 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 37 degree C pre-incubated for 30 mins followed by carbachol addition and measured after 60 mins by HTRF assayAntagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 37 degree C pre-incubated for 30 mins followed by carbachol addition and measured after 60 mins by HTRF assay
ChEMBL 1968 45 8 21 14.3 CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCc3cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)cc(C(=O)NCCNC(=O)CCc4cn(CCCCC5CCN(CC(=O)N6c7ccccc7NC(=O)c7ccccc76)CC5)cn4)c3)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21 10.1021/acs.jmedchem.9b02172
CHEMBL4851711 183966 0 None -1318 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccccc1-c1ccc(N[C@H]2C[C@@H]3CN(CC4CCOCC4)C[C@@H]3C2)nn1 10.1021/acsmedchemlett.1c00363
44265375 201692 0 None -3 2 Rat 6.6 pIC50 = 6.6 Functional
Muscarinic receptor M2 in rat heart using [3H]QNB (quinuclidinyl benzylate) radioligand as a M2 non-selective muscarinic receptor antagonist at a concentration of 0.12 nMMuscarinic receptor M2 in rat heart using [3H]QNB (quinuclidinyl benzylate) radioligand as a M2 non-selective muscarinic receptor antagonist at a concentration of 0.12 nM
ChEMBL 208 2 0 4 0.8 C(#CCN1CCCC1)COC1=NOCC1 10.1016/S0960-894X(97)00150-9
CHEMBL8610 201692 0 None -3 2 Rat 6.6 pIC50 = 6.6 Functional
Muscarinic receptor M2 in rat heart using [3H]QNB (quinuclidinyl benzylate) radioligand as a M2 non-selective muscarinic receptor antagonist at a concentration of 0.12 nMMuscarinic receptor M2 in rat heart using [3H]QNB (quinuclidinyl benzylate) radioligand as a M2 non-selective muscarinic receptor antagonist at a concentration of 0.12 nM
ChEMBL 208 2 0 4 0.8 C(#CCN1CCCC1)COC1=NOCC1 10.1016/S0960-894X(97)00150-9
CHEMBL4758635 180142 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 300 3 0 2 3.6 C[C@H]1CCC[C@@H](C)N1C(=O)CCN1CCCc2ccccc21 10.1016/j.bmcl.2020.127632
CHEMBL3084678 102713 0 None 1 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human cloned muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M2 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
CHEMBL4787283 181696 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 272 2 0 2 2.8 Cc1ccc2c(c1)CCCN2CC(=O)N1CCCCC1 10.1016/j.bmcl.2020.127632
44418764 81539 0 None -1 4 Human 6.6 pIC50 = 6.6 Functional
Activity at human M2 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M2 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
CHEMBL216928 81539 0 None -1 4 Human 6.6 pIC50 = 6.6 Functional
Activity at human M2 receptor assessed as inhibition of forskolin-stimulated cAMP accumulationActivity at human M2 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
44590033 182841 0 None -12 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 182841 0 None -12 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
44590166 188565 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 188565 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
CHEMBL3085076 102798 0 None -3 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
10220392 201552 0 None -6 2 Human 4.6 pIC50 = 4.6 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 240 2 0 3 1.7 C(#Cc1ccccc1)CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL84893 201552 0 None -6 2 Human 4.6 pIC50 = 4.6 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 240 2 0 3 1.7 C(#Cc1ccccc1)CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL3085089 102812 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
CHEMBL4855467 184225 0 None -1737 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 435 6 2 6 3.7 CC(=O)Nc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
CHEMBL4860985 184563 0 None -338 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1ccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)cc1 10.1021/acsmedchemlett.1c00363
137630050 160237 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Competitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 10 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF assayCompetitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 10 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF 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 160237 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Competitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 10 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF assayCompetitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 10 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF 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 160237 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Competitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 10 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF assayCompetitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 10 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF 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 160237 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Competitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 10 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF assayCompetitive antagonist activity at human muscarinic acetylcholine receptor M2 expressed in HEK293 cells coexpressing HA tagged Galpha-protein qi5 assessed as inhibition of 10 uM carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition measured after 1 hr by HTRF 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
46830362 7650 0 None -5 5 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)ccc3C(F)(F)F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1090097 7650 0 None -5 5 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M2 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)ccc3C(F)(F)F)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL3085092 102815 0 None -2 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
CHEMBL4861863 185391 0 None -870 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
CHEMBL4873386 185391 0 None -870 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 5 4.5 Fc1ccc(Cl)c(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
9990434 105643 0 None 1 3 Human 5.6 pIC50 = 5.6 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 202 2 0 3 0.7 C#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL313918 105643 0 None 1 3 Human 5.6 pIC50 = 5.6 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 202 2 0 3 0.7 C#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
44455159 97105 0 None -25 5 Rat 4.5 pIC50 = 4.5 Functional
Antagonist activity at rat muscarinic M2 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M2 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 97105 0 None -25 5 Rat 4.5 pIC50 = 4.5 Functional
Antagonist activity at rat muscarinic M2 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M2 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
46682613 180318 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 286 4 1 2 3.3 O=C(CCN1CCCc2ccccc21)NC1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4760823 180318 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 286 4 1 2 3.3 O=C(CCN1CCCc2ccccc21)NC1CCCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4792360 182074 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 288 3 1 3 1.8 O=C(CCN1CCCc2ccccc21)N1CCCC(O)C1 10.1016/j.bmcl.2020.127632
44590174 169241 0 None 3 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 169241 0 None 3 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 169241 0 None 3 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
44590178 171920 0 None 1 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 171920 0 None 1 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 171920 0 None 1 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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
CHEMBL3085060 105802 0 None -11 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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 105802 0 None -11 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at cloned muscarinic M2 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M2 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
CHEMBL4854289 184149 0 None -1318 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 396 5 1 5 3.8 Fc1cccc(-c2ccc(N[C@H]3C[C@@H]4CN(CC5CCOCC5)C[C@@H]4C3)nn2)c1 10.1021/acsmedchemlett.1c00363
10058347 105238 0 None -2 2 Human 4.5 pIC50 = 4.5 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 190 3 0 3 0.9 C#C/C=C/CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL312823 105238 0 None -2 2 Human 4.5 pIC50 = 4.5 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 190 3 0 3 0.9 C#C/C=C/CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
71450615 83306 0 None -1 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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 83306 0 None -1 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M2 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
11819427 57059 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 168 2 0 3 1.1 CC(C)O/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL166423 57059 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cellsInhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells
ChEMBL 168 2 0 3 1.1 CC(C)O/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
47358375 179924 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 272 4 1 2 2.9 O=C(CCN1CCCc2ccccc21)NC1CCCC1 10.1016/j.bmcl.2020.127632
CHEMBL4756164 179924 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholineAntagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
ChEMBL 272 4 1 2 2.9 O=C(CCN1CCCc2ccccc21)NC1CCCC1 10.1016/j.bmcl.2020.127632
11584660 92625 5 None -1 5 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic receptor M2Antagonist activity at human muscarinic receptor M2
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
CHEMBL244946 92625 5 None -1 5 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human muscarinic receptor M2Antagonist activity at human muscarinic receptor M2
ChEMBL 537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1 10.1021/jm0705612
44590182 182314 0 None -12 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 182314 0 None -12 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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 189038 0 None -12 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M2 receptor expressed in CHO cells coexpressing chimeric G protein Gqi5 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