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 205433 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 205433 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 2020 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 2020 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 2020 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
42599070 15887 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
CHEMBL1223804 15887 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 160557 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 160557 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 160557 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 160609 13 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 160609 13 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 160609 13 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 461 55 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
296 461 55 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 461 55 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 461 55 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 780 23 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
298 780 23 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
488 780 23 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 780 23 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 780 23 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 10427 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 10427 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 4116 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 4116 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 160461 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 160461 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 160461 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 110909 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 110909 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 184696 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 184696 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 186470 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 186470 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 780 23 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
298 780 23 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
488 780 23 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 780 23 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 780 23 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 21422 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 21422 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 160461 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 160461 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 160461 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 123082 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 123082 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 160417 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 160417 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 160417 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 4022 72 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 4022 72 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 4022 72 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 4022 72 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 4022 72 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 199139 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 199139 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
42598829 15889 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
CHEMBL1223806 15889 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 157251 28 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 157251 28 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 206678 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 206678 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 59229 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 59229 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 200252 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 200252 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 201415 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 201415 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
122189496 122807 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
CHEMBL3616500 122807 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 155329 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 155329 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 73949 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 73949 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 160615 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 160615 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 160615 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 205433 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 205433 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
24967746 15864 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
CHEMBL1223754 15864 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 116262 3 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 116262 3 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 4110 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 4110 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 164067 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 164067 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 160461 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 160461 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 160461 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 123083 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 123083 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 155530 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 155530 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
187 253 34 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
294 253 34 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
65 253 34 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 253 34 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 253 34 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 253 34 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
187 253 34 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
294 253 34 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
65 253 34 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 253 34 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 253 34 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 253 34 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 160533 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 160533 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 160533 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 172652 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 172652 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 107221 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 107221 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 200329 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 200329 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 160591 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 160591 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 160591 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 160434 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 160434 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 160434 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
122189499 122808 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
CHEMBL3616504 122808 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 100059 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 100059 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 100059 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 100059 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
122191007 123086 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
CHEMBL3618449 123086 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
42598357 15914 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
CHEMBL1223863 15914 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
42598359 15915 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
CHEMBL1223864 15915 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
25207745 15935 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
CHEMBL1223941 15935 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 156567 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 156567 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 203923 4 None -162 6 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 203923 4 None -162 6 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 100134 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 100134 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 160451 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 160451 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 160451 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 23927 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 23927 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 188075 40 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 188075 40 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 203923 4 None -162 6 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 203923 4 None -162 6 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 54114 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 54114 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 54114 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 188075 40 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 188075 40 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 172653 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 172653 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 158742 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 158742 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 21156 27 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 21156 27 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 205433 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 205433 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 160461 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 160461 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 160461 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 160461 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 160461 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 160461 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
122191006 123085 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
CHEMBL3618448 123085 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 4022 72 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 4022 72 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 4022 72 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 4022 72 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 4022 72 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
42598360 15913 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
CHEMBL1223862 15913 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 97617 23 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 97617 23 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 97617 23 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 122804 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 122804 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 123081 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 123081 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
187 253 34 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
294 253 34 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
65 253 34 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 253 34 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 253 34 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 253 34 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 27097 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 27097 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
187 253 34 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
294 253 34 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
65 253 34 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 253 34 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 253 34 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 253 34 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 156150 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 156150 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
42598358 15911 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
CHEMBL1223860 15911 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
187 253 34 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
294 253 34 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
65 253 34 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 253 34 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 253 34 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 253 34 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
187 253 34 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
294 253 34 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
65 253 34 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 253 34 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 253 34 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 253 34 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 199731 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 199731 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 85872 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 85872 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
187 253 34 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
294 253 34 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
65 253 34 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 253 34 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 253 34 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 253 34 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
122191005 123084 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
CHEMBL3618447 123084 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 780 23 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
298 780 23 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
488 780 23 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 780 23 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 780 23 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 2788 4 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 2788 4 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 2788 4 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 3387 18 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 3387 18 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 3387 18 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 3387 18 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 3387 18 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
42598591 15886 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
CHEMBL1223803 15886 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
42599068 15888 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
CHEMBL1223805 15888 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
25230693 15934 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
CHEMBL1223940 15934 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 15863 15 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 15863 15 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 80033 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 80033 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 80034 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 80034 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 160417 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 160417 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 160417 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 3062 46 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 3062 46 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 3062 46 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 3062 46 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 3062 46 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 160417 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 160417 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 160417 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
122189495 122806 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
CHEMBL3616499 122806 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
122191008 123087 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
CHEMBL3618450 123087 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 101805 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 101805 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 21422 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 21422 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 102140 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 102140 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
5441 2383 5 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 O[C@@H]1Cc2c([C@H]1NC(=O)c1ccc(cc1)c1ccccc1)cc(cc2)N=C(N(Cc1ccc(cc1)F)C)C 10.1016/j.bmcl.2015.08.011
9893054 2383 5 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 O[C@@H]1Cc2c([C@H]1NC(=O)c1ccc(cc1)c1ccccc1)cc(cc2)N=C(N(Cc1ccc(cc1)F)C)C 10.1016/j.bmcl.2015.08.011
CHEMBL3616501 2383 5 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 O[C@@H]1Cc2c([C@H]1NC(=O)c1ccc(cc1)c1ccccc1)cc(cc2)N=C(N(Cc1ccc(cc1)F)C)C 10.1016/j.bmcl.2015.08.011
187 253 34 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
294 253 34 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
65 253 34 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 253 34 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 253 34 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 253 34 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 780 23 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
298 780 23 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
488 780 23 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 780 23 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 780 23 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 780 23 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
298 780 23 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
488 780 23 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 780 23 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 780 23 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 123077 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 123077 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 123074 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 123074 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 199461 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 199461 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 160417 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 160417 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 160417 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 199623 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 199623 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 199623 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 199623 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 160417 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 160417 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 160417 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 80032 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 80032 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 100466 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 100466 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 15863 15 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 15863 15 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
42598828 15912 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
CHEMBL1223861 15912 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
42599071 15933 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
CHEMBL1223939 15933 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 100058 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 100058 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 100058 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 199541 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 199541 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 156445 57 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 156445 57 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 162679 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 162679 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 21422 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 21422 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 77983 32 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 77983 32 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 162449 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 162449 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 780 23 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
298 780 23 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
488 780 23 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 780 23 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 780 23 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 206412 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 206412 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 100453 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 100453 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 160616 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 160616 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 160616 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 40156 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 40156 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 55649 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 55649 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 55649 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 157238 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 157238 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 156403 20 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 156403 20 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
44372610 52248 0 None 181 2 Human 9.1 pED50 = 9.1 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 340 5 0 5 2.7 COc1ccc(C#C/C(C)=C\CO/N=C2/CN3CCC2C3)cc1OC 10.1016/0960-894X(95)00087-A
CHEMBL159208 52248 0 None 181 2 Human 9.1 pED50 = 9.1 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 340 5 0 5 2.7 COc1ccc(C#C/C(C)=C\CO/N=C2/CN3CCC2C3)cc1OC 10.1016/0960-894X(95)00087-A
44372301 49518 0 None 40 2 Human 8.7 pED50 = 8.7 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 340 5 0 5 2.7 COc1ccc(C#C/C(C)=C/CO/N=C2\CN3CCC2C3)cc1OC 10.1016/0960-894X(95)00087-A
CHEMBL156749 49518 0 None 40 2 Human 8.7 pED50 = 8.7 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 340 5 0 5 2.7 COc1ccc(C#C/C(C)=C/CO/N=C2\CN3CCC2C3)cc1OC 10.1016/0960-894X(95)00087-A
44372633 50022 0 None -1 2 Human 8.0 pED50 = 8.0 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 310 4 0 4 2.7 COc1ccc(C#C/C(C)=C\CO/N=C2/CN3CCC2C3)cc1 10.1016/0960-894X(95)00087-A
CHEMBL157197 50022 0 None -1 2 Human 8.0 pED50 = 8.0 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 310 4 0 4 2.7 COc1ccc(C#C/C(C)=C\CO/N=C2/CN3CCC2C3)cc1 10.1016/0960-894X(95)00087-A
44372232 119302 0 None - 0 Human 8.0 pED50 = 8.0 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 294 3 0 3 3.0 C/C(C#Cc1ccc(C)cc1)=C/CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL348412 119302 0 None - 0 Human 8.0 pED50 = 8.0 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 294 3 0 3 3.0 C/C(C#Cc1ccc(C)cc1)=C/CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
10058744 204647 0 None 1 2 Human 8.0 pED50 = 8.0 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 204 3 0 3 1.3 C#C/C(C)=C/CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL87622 204647 0 None 1 2 Human 8.0 pED50 = 8.0 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 204 3 0 3 1.3 C#C/C(C)=C/CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
44372253 49725 0 None 21 2 Human 7.9 pED50 = 7.9 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 310 4 0 4 2.7 COc1cccc(C#C/C(C)=C/CO/N=C2/CN3CCC2C3)c1 10.1016/0960-894X(95)00087-A
CHEMBL156925 49725 0 None 21 2 Human 7.9 pED50 = 7.9 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 310 4 0 4 2.7 COc1cccc(C#C/C(C)=C/CO/N=C2/CN3CCC2C3)c1 10.1016/0960-894X(95)00087-A
9795428 96028 4 None -30 5 Human 5.9 pED50 = 5.9 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M2 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M2 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
CHEMBL262455 96028 4 None -30 5 Human 5.9 pED50 = 5.9 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M2 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M2 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
5487543 203923 4 None -162 6 Human 5.9 pED50 = 5.9 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M2 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M2 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
CHEMBL81878 203923 4 None -162 6 Human 5.9 pED50 = 5.9 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M2 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M2 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
10266025 119648 0 None - 0 Human 8.6 pED50 = 8.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 286 3 0 4 2.8 C/C(C#Cc1cccs1)=C/CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL351561 119648 0 None - 0 Human 8.6 pED50 = 8.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 286 3 0 4 2.8 C/C(C#Cc1cccs1)=C/CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
44372580 119263 0 None - 0 Human 8.6 pED50 = 8.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 286 3 0 4 2.8 C/C(C#Cc1cccs1)=C/CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL348079 119263 0 None - 0 Human 8.6 pED50 = 8.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 286 3 0 4 2.8 C/C(C#Cc1cccs1)=C/CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
44372492 155171 0 None - 0 Human 8.6 pED50 = 8.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 314 3 0 3 3.3 C/C(C#Cc1ccc(Cl)cc1)=C/CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL405426 155171 0 None - 0 Human 8.6 pED50 = 8.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 314 3 0 3 3.3 C/C(C#Cc1ccc(Cl)cc1)=C/CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
2551 780 23 None -2 12 Human 7.6 pED50 = 7.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/0960-894X(95)00087-A
298 780 23 None -2 12 Human 7.6 pED50 = 7.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/0960-894X(95)00087-A
488 780 23 None -2 12 Human 7.6 pED50 = 7.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/0960-894X(95)00087-A
CHEMBL965 780 23 None -2 12 Human 7.6 pED50 = 7.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/0960-894X(95)00087-A
DB00411 780 23 None -2 12 Human 7.6 pED50 = 7.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/0960-894X(95)00087-A
10420458 204535 0 None 7 2 Human 7.6 pED50 = 7.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 204 3 0 3 1.3 C#C/C(C)=C\CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL86903 204535 0 None 7 2 Human 7.6 pED50 = 7.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 204 3 0 3 1.3 C#C/C(C)=C\CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
44372591 54045 0 None -60 2 Human 7.6 pED50 = 7.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 286 3 0 4 2.8 C/C(C#Cc1cccs1)=C\CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL160858 54045 0 None -60 2 Human 7.6 pED50 = 7.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 286 3 0 4 2.8 C/C(C#Cc1cccs1)=C\CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
44372290 54151 0 None -5 2 Human 6.6 pED50 = 6.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 298 3 0 3 2.8 C/C(C#Cc1ccc(F)cc1)=C/CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL160939 54151 0 None -5 2 Human 6.6 pED50 = 6.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 298 3 0 3 2.8 C/C(C#Cc1ccc(F)cc1)=C/CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
2551 780 23 None -2 12 Human 6.6 pED50 = 6.6 Functional
Binding affinity expressed in IC50 labelled by [3H]QNB in CHO cells expressing human Muscarinic acetylcholine receptor M2Binding affinity expressed in IC50 labelled by [3H]QNB in CHO cells expressing human Muscarinic acetylcholine receptor M2
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
298 780 23 None -2 12 Human 6.6 pED50 = 6.6 Functional
Binding affinity expressed in IC50 labelled by [3H]QNB in CHO cells expressing human Muscarinic acetylcholine receptor M2Binding affinity expressed in IC50 labelled by [3H]QNB in CHO cells expressing human Muscarinic acetylcholine receptor M2
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
488 780 23 None -2 12 Human 6.6 pED50 = 6.6 Functional
Binding affinity expressed in IC50 labelled by [3H]QNB in CHO cells expressing human Muscarinic acetylcholine receptor M2Binding affinity expressed in IC50 labelled by [3H]QNB in CHO cells expressing human Muscarinic acetylcholine receptor M2
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
CHEMBL965 780 23 None -2 12 Human 6.6 pED50 = 6.6 Functional
Binding affinity expressed in IC50 labelled by [3H]QNB in CHO cells expressing human Muscarinic acetylcholine receptor M2Binding affinity expressed in IC50 labelled by [3H]QNB in CHO cells expressing human Muscarinic acetylcholine receptor M2
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
DB00411 780 23 None -2 12 Human 6.6 pED50 = 6.6 Functional
Binding affinity expressed in IC50 labelled by [3H]QNB in CHO cells expressing human Muscarinic acetylcholine receptor M2Binding affinity expressed in IC50 labelled by [3H]QNB in CHO cells expressing human Muscarinic acetylcholine receptor M2
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
44372254 53667 0 None - 1 Human 7.6 pED50 = 7.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 310 4 0 4 2.7 COc1cccc(C#C/C(C)=C\CO/N=C2/CN3CCC2C3)c1 10.1016/0960-894X(95)00087-A
CHEMBL160554 53667 0 None - 1 Human 7.6 pED50 = 7.6 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 310 4 0 4 2.7 COc1cccc(C#C/C(C)=C\CO/N=C2/CN3CCC2C3)c1 10.1016/0960-894X(95)00087-A
10086044 48698 0 None 6 2 Human 8.5 pED50 = 8.5 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 298 3 0 3 2.8 C/C(C#Cc1ccc(F)cc1)=C/CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL156050 48698 0 None 6 2 Human 8.5 pED50 = 8.5 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 298 3 0 3 2.8 C/C(C#Cc1ccc(F)cc1)=C/CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
9903828 118975 0 None 28 2 Human 8.4 pED50 = 8.4 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 280 3 0 3 2.7 C/C(C#Cc1ccccc1)=C/CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL345415 118975 0 None 28 2 Human 8.4 pED50 = 8.4 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 280 3 0 3 2.7 C/C(C#Cc1ccccc1)=C/CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
44372506 118951 0 None 19 2 Human 8.4 pED50 = 8.4 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 294 3 0 3 3.0 C/C(C#Cc1ccc(C)cc1)=C/CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL345205 118951 0 None 19 2 Human 8.4 pED50 = 8.4 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 294 3 0 3 3.0 C/C(C#Cc1ccc(C)cc1)=C/CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
44372278 49130 0 None 11 2 Human 8.4 pED50 = 8.4 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 310 4 0 4 2.7 COc1cccc(C#C/C(C)=C\CO/N=C2\CN3CCC2C3)c1 10.1016/0960-894X(95)00087-A
CHEMBL156445 49130 0 None 11 2 Human 8.4 pED50 = 8.4 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 310 4 0 4 2.7 COc1cccc(C#C/C(C)=C\CO/N=C2\CN3CCC2C3)c1 10.1016/0960-894X(95)00087-A
44372277 167789 0 None - 0 Human 7.4 pED50 = 7.4 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 310 4 0 4 2.7 COc1cccc(C#C/C(C)=C/CO/N=C2\CN3CCC2C3)c1 10.1016/0960-894X(95)00087-A
CHEMBL434469 167789 0 None - 0 Human 7.4 pED50 = 7.4 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 310 4 0 4 2.7 COc1cccc(C#C/C(C)=C/CO/N=C2\CN3CCC2C3)c1 10.1016/0960-894X(95)00087-A
10242016 167725 0 None - 0 Human 7.4 pED50 = 7.4 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 204 3 0 3 1.3 C#C/C(C)=C\CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL434072 167725 0 None - 0 Human 7.4 pED50 = 7.4 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 204 3 0 3 1.3 C#C/C(C)=C\CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
44372289 118958 0 None -2 2 Human 6.3 pED50 = 6.3 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 298 3 0 3 2.8 C/C(C#Cc1ccc(F)cc1)=C\CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL345250 118958 0 None -2 2 Human 6.3 pED50 = 6.3 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 298 3 0 3 2.8 C/C(C#Cc1ccc(F)cc1)=C\CO/N=C1/CN2CCC1C2 10.1016/0960-894X(95)00087-A
44213237 101438 0 None - 0 Human 6.2 pED50 = 6.2 Functional
Effective dose against affinity towards human muscarinic M2 receptorEffective dose against affinity towards human muscarinic M2 receptor
ChEMBL 291 8 0 5 2.5 CCCCCCOc1nccnc1OC1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL300998 101438 0 None - 0 Human 6.2 pED50 = 6.2 Functional
Effective dose against affinity towards human muscarinic M2 receptorEffective dose against affinity towards human muscarinic M2 receptor
ChEMBL 291 8 0 5 2.5 CCCCCCOc1nccnc1OC1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
44372647 119502 0 None -1 2 Human 8.1 pED50 = 8.1 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 310 4 0 4 2.7 COc1ccc(C#C/C(C)=C\CO/N=C2\CN3CCC2C3)cc1 10.1016/0960-894X(95)00087-A
CHEMBL350223 119502 0 None -1 2 Human 8.1 pED50 = 8.1 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 310 4 0 4 2.7 COc1ccc(C#C/C(C)=C\CO/N=C2\CN3CCC2C3)cc1 10.1016/0960-894X(95)00087-A
44371814 51109 0 None 3 2 Human 8.0 pED50 = 8.0 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 298 3 0 3 2.8 C/C(C#Cc1ccc(F)cc1)=C\CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL158180 51109 0 None 3 2 Human 8.0 pED50 = 8.0 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 298 3 0 3 2.8 C/C(C#Cc1ccc(F)cc1)=C\CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
44372452 119105 0 None - 0 Human 6.0 pED50 = 6.0 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 348 3 0 3 4.0 C/C(C#Cc1ccc(Cl)c(Cl)c1)=C\CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
CHEMBL346580 119105 0 None - 0 Human 6.0 pED50 = 6.0 Functional
Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.Agonistic efficacy in human m2 muscarinic receptor expressed with the marker gene beta-galactosidase in NIH 3T3 cells.
ChEMBL 348 3 0 3 4.0 C/C(C#Cc1ccc(Cl)c(Cl)c1)=C\CO/N=C1\CN2CCC1C2 10.1016/0960-894X(95)00087-A
9913341 81732 3 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 81732 3 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 81732 3 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 169739 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 169739 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 169739 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 178161 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 178161 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 178161 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 188467 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 188467 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 188467 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 175996 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 175996 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 175996 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
11690968 106006 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
CHEMBL3085072 106006 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 106006 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 172138 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 172138 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 172138 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 178436 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 178436 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 185388 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 185388 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 191951 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 191951 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 84226 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 84226 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+
76313456 106014 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
CHEMBL3085066 106014 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 106014 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
162675053 182666 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
CHEMBL4796491 182666 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 83498 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 83498 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 106566 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 106566 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 86125 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 86125 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
162353372 180795 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
CHEMBL4763422 180795 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 83506 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 83506 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 86125 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 86125 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 181226 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 181226 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
76327901 103007 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
CHEMBL3085084 103007 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
44233675 102890 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
CHEMBL3084639 102890 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
11518068 106011 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
CHEMBL3085059 106011 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 106011 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 172067 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 172067 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 172067 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 188037 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 188037 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 188037 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 158473 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 158473 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
162353379 180370 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
CHEMBL4758449 180370 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 192805 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 192805 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 183268 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 183268 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 192805 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 192805 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 174711 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 174711 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
44233417 85605 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
CHEMBL2307674 85605 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 192461 51 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 192461 51 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 192461 51 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 192461 51 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 2428 4 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 2428 4 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 2428 4 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 2428 4 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 2428 4 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 83505 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 83505 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
11503336 106019 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
CHEMBL3085071 106019 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 106019 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
76309756 103006 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
CHEMBL3085083 103006 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
76313457 103003 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
CHEMBL3085080 103003 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 204301 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 204301 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
162353393 178849 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
CHEMBL4740422 178849 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 84464 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 84464 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+
76320693 103005 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
CHEMBL3085082 103005 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 179883 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 179883 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
76309755 103001 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
CHEMBL3085079 103001 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
76320692 106013 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
CHEMBL3085065 106013 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 106013 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 83504 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 83504 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 187777 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 187777 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 187777 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 182283 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 182283 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
162353369 180203 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
CHEMBL4756442 180203 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
44232953 102903 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
CHEMBL3084663 102903 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 119801 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 119801 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 188169 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 188169 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 188169 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 188169 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 189954 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 189954 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 191148 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 191148 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 187818 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 187818 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 172008 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 172008 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 172178 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 172178 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 58672 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 58672 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 160481 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 160481 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 160481 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 160481 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
137408729 190138 0 None -870 2 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human muscarinic acetylcholine M2 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M2 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 444 6 1 5 4.9 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5182783 190138 0 None -870 2 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human muscarinic acetylcholine M2 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M2 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 444 6 1 5 4.9 Fc1ccc(Cl)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
15681299 119960 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 119960 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 177738 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 177738 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 177738 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 120191 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 120191 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 160481 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 160481 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 160481 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 160481 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
162353388 180387 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
CHEMBL4758633 180387 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 83488 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 83488 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
168276820 189503 0 None -63 2 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human muscarinic acetylcholine M2 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M2 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5172967 189503 0 None -63 2 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human muscarinic acetylcholine M2 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M2 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
CHEMBL5208649 189503 0 None -63 2 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human muscarinic acetylcholine M2 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assayInhibition of human muscarinic acetylcholine M2 receptor expressed in CHO cells co-expressing Gqi5 in the presence of acetylcholine at EC80 concentration by calcium mobilization assay
ChEMBL 446 6 1 5 4.5 Fc1cc(F)c(F)c(-c2ccc(NC[C@@H]3CC34CCN(CC3CCOCC3)CC4)nn2)c1 10.1016/j.bmcl.2021.128479
71454215 83497 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 83497 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 179544 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 cell