Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
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
9927975 4125 0 None 10 2 Human 9.7 pEC50 = 9.7 Functional
Effective concentration required for stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorEffective concentration required for stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 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 4125 0 None 10 2 Human 9.7 pEC50 = 9.7 Functional
Effective concentration required for stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorEffective concentration required for stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 341 3 0 5 3.5 C(#Cc1ccccc1)CSc1nsnc1[C@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
24967746 15879 0 None 31 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223754 15879 0 None 31 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42599070 15902 0 None 50 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223804 15902 0 None 50 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
44330081 206422 0 None 17 2 Human 9.3 pEC50 = 9.3 Functional
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 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 206422 0 None 17 2 Human 9.3 pEC50 = 9.3 Functional
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
42598591 15901 0 None 39 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223803 15901 0 None 39 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
118724611 115961 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 373 3 1 5 3.4 Cn1cc(-c2ccc(Cn3cc4c(=O)[nH]nc-4c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2014.11.011
CHEMBL3360954 115961 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 373 3 1 5 3.4 Cn1cc(-c2ccc(Cn3cc4c(=O)[nH]nc-4c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2014.11.011
25110765 186435 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccc(F)cc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL490797 186435 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccc(F)cc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
46871844 6734 0 None 50 5 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083925 6734 0 None 50 5 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
25110764 192469 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(F)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL522451 192469 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(F)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
44329977 110922 0 None 10 2 Human 9.0 pEC50 = 9 Functional
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC1C2 10.1016/s0960-894x(98)00509-5
CHEMBL327269 110922 0 None 10 2 Human 9.0 pEC50 = 9 Functional
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC1C2 10.1016/s0960-894x(98)00509-5
46890906 6964 0 None 1 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 329 5 2 2 4.8 OC(CCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1084850 6964 0 None 1 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 329 5 2 2 4.8 OC(CCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
42598358 15926 0 None 50 5 Human 9.0 pEC50 = 9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223860 15926 0 None 50 5 Human 9.0 pEC50 = 9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
44351242 117557 0 None 5 2 Human 9.0 pEC50 = 9 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 285 5 0 6 2.5 CCCSc1nsnc1OC1CN2CCCC1C2 10.1021/jm970125n
CHEMBL340435 117557 0 None 5 2 Human 9.0 pEC50 = 9 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 285 5 0 6 2.5 CCCSc1nsnc1OC1CN2CCCC1C2 10.1021/jm970125n
44330074 106723 0 None - 1 Human 9.0 pEC50 = 9 Functional
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 341 3 0 5 3.5 C(#Cc1ccccc1)CSc1nsnc1[C@@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL316625 106723 0 None - 1 Human 9.0 pEC50 = 9 Functional
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 341 3 0 5 3.5 C(#Cc1ccccc1)CSc1nsnc1[C@@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
44579457 186279 0 None 2570 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 476 4 1 4 4.8 O=c1[nH]c2cc(F)ccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL489576 186279 0 None 2570 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 476 4 1 4 4.8 O=c1[nH]c2cc(F)ccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
44579418 186399 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4c(F)cccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL490598 186399 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4c(F)cccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
187 253 34 None -10 6 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 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 -10 6 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 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 -10 6 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 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 -10 6 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 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 -10 6 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 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 -10 6 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 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 -10 6 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
294 253 34 None -10 6 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
65 253 34 None -10 6 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
8593 253 34 None -10 6 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
CHEMBL667 253 34 None -10 6 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
DB03128 253 34 None -10 6 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
9883040 100071 0 None 3 3 Human 9.0 pEC50 = 9.0 Functional
In vitro functional agonism against M1 muscarinic receptor (PI)In vitro functional agonism against M1 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL291339 100071 0 None 3 3 Human 9.0 pEC50 = 9.0 Functional
In vitro functional agonism against M1 muscarinic receptor (PI)In vitro functional agonism against M1 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL542622 100071 0 None 3 3 Human 9.0 pEC50 = 9.0 Functional
In vitro functional agonism against M1 muscarinic receptor (PI)In vitro functional agonism against M1 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
68153829 115962 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 341 3 1 5 3.1 O=c1[nH]nc2c3ccccc3n(Cc3ccc(-n4cccn4)cc3)cc1-2 10.1016/j.bmcl.2014.11.011
CHEMBL3360955 115962 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 341 3 1 5 3.1 O=c1[nH]nc2c3ccccc3n(Cc3ccc(-n4cccn4)cc3)cc1-2 10.1016/j.bmcl.2014.11.011
42598828 15927 0 None 125 5 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223861 15927 0 None 125 5 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
302 2929 23 None -3 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1016/j.bmcl.2015.02.012
4630 2929 23 None -3 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1016/j.bmcl.2015.02.012
CHEMBL7634 2929 23 None -3 8 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1016/j.bmcl.2015.02.012
3652 4034 72 None -21 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57 4034 72 None -21 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809 4034 72 None -21 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
CHEMBL21536 4034 72 None -21 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
DB15357 4034 72 None -21 9 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
44579419 192084 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 476 4 1 4 4.8 O=c1[nH]c2c(F)cccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL521914 192084 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 476 4 1 4 4.8 O=c1[nH]c2c(F)cccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
24751745 198173 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assayAgonist activity at human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assay
ChEMBL 345 4 1 4 3.0 COc1ccc(Cn2cc(C(=O)O)c(=O)c3c(F)ccc(F)c32)cc1 10.1021/jm400540b
CHEMBL594432 198173 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assayAgonist activity at human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assay
ChEMBL 345 4 1 4 3.0 COc1ccc(Cn2cc(C(=O)O)c(=O)c3c(F)ccc(F)c32)cc1 10.1021/jm400540b
22730942 17922 0 None -2 2 Human 8.7 pEC50 = 8.7 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 271 5 0 6 2.1 CCCSc1nsnc1OC1CN2CCC1C2 10.1021/jm970125n
CHEMBL126846 17922 0 None -2 2 Human 8.7 pEC50 = 8.7 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 271 5 0 6 2.1 CCCSc1nsnc1OC1CN2CCC1C2 10.1021/jm970125n
9809330 115499 0 None -39 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0606995
CHEMBL335542 115499 0 None -39 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0606995
46891179 6340 0 None 251 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 378 4 2 2 4.2 C[C@H]1CNCC[C@]1(F)CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1082365 6340 0 None 251 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 378 4 2 2 4.2 C[C@H]1CNCC[C@]1(F)CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46871665 6517 0 None 100 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1F 10.1016/j.bmcl.2010.04.128
CHEMBL1083108 6517 0 None 100 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1F 10.1016/j.bmcl.2010.04.128
25207745 15950 0 None 79 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223941 15950 0 None 79 5 Human 8.0 pEC50 = 8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
46930343 16522 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 381 6 1 4 2.1 CCC(=O)NC1CCN(CCCN2C(=O)COc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
CHEMBL1242925 16522 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 381 6 1 4 2.1 CCC(=O)NC1CCN(CCCN2C(=O)COc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
264734 10015 70 None - 1 Human 8.0 pEC50 = 8 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 237 2 0 2 2.4 O=C1C(=O)N(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2014.11.011
CHEMBL115581 10015 70 None - 1 Human 8.0 pEC50 = 8 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 237 2 0 2 2.4 O=C1C(=O)N(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2014.11.011
118724612 115963 0 None - 1 Human 8.0 pEC50 = 8 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 303 3 0 4 2.6 O=C1C(=O)N(Cc2ccc(-n3cccn3)cc2)c2ccccc21 10.1016/j.bmcl.2014.11.011
CHEMBL3360956 115963 0 None - 1 Human 8.0 pEC50 = 8 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 303 3 0 4 2.6 O=C1C(=O)N(Cc2ccc(-n3cccn3)cc2)c2ccccc21 10.1016/j.bmcl.2014.11.011
44303018 200338 0 None 4 3 Human 8.0 pEC50 = 8.0 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 343 3 0 5 2.4 Clc1cccc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL60833 200338 0 None 4 3 Human 8.0 pEC50 = 8.0 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 343 3 0 5 2.4 Clc1cccc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
46891597 6321 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 362 4 2 2 4.4 O=C(NCC1CCNCC1)c1ccc(Cl)cc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1082316 6321 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 362 4 2 2 4.4 O=C(NCC1CCNCC1)c1ccc(Cl)cc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46890714 6539 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 362 4 2 2 4.4 O=C(NCC1CCNCC1)c1cc(Cl)ccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083277 6539 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 362 4 2 2 4.4 O=C(NCC1CCNCC1)c1cc(Cl)ccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
44207208 16540 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 423 7 1 4 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CSc3ccccc32)CC1 10.1021/jm100697g
CHEMBL1243138 16540 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 423 7 1 4 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CSc3ccccc32)CC1 10.1021/jm100697g
145984661 164827 0 None -8 2 Rat 7.0 pEC50 = 7 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 448 5 2 7 3.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)N[C@@H]3CCOC[C@H]3O)nc21 10.1021/acsmedchemlett.8b00261
CHEMBL4237601 164827 0 None -8 2 Rat 7.0 pEC50 = 7 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 448 5 2 7 3.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)N[C@@H]3CCOC[C@H]3O)nc21 10.1021/acsmedchemlett.8b00261
16094783 136044 0 None -12 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL373888 136044 0 None -12 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
70685587 73828 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 5 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cccs1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2022948 73828 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 5 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cccs1)C2 10.1016/j.bmcl.2012.03.088
76327871 102795 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 4 2.1 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)C1CCCCC1 10.1016/j.bmcl.2012.03.088
CHEMBL3084452 102795 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 4 2.1 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)C1CCCCC1 10.1016/j.bmcl.2012.03.088
46890718 6652 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2cccc(Cl)c2)c(C(=O)NCC2CCNCC2)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083718 6652 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2cccc(Cl)c2)c(C(=O)NCC2CCNCC2)c1 10.1016/j.bmcl.2010.04.127
46890972 6890 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1F 10.1016/j.bmcl.2010.04.128
CHEMBL1084572 6890 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1F 10.1016/j.bmcl.2010.04.128
46890907 6965 0 None -79 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 311 4 1 1 5.4 Clc1cccc(-c2ccccc2/C=C/CC2CCNCC2)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1084851 6965 0 None -79 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 311 4 1 1 5.4 Clc1cccc(-c2ccccc2/C=C/CC2CCNCC2)c1 10.1016/j.bmcl.2010.04.127
20918653 115949 5 None - 1 Human 6.0 pEC50 = 6 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 383 4 0 4 4.5 O=c1c2cn(Cc3ccccc3)c3ccccc3c-2nn1Cc1ccccc1F 10.1016/j.bmcl.2014.11.011
CHEMBL3360928 115949 5 None - 1 Human 6.0 pEC50 = 6 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 383 4 0 4 4.5 O=c1c2cn(Cc3ccccc3)c3ccccc3c-2nn1Cc1ccccc1F 10.1016/j.bmcl.2014.11.011
187 253 34 None -10 6 Human 4.0 pEC50 = 4 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.02.012
294 253 34 None -10 6 Human 4.0 pEC50 = 4 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.02.012
65 253 34 None -10 6 Human 4.0 pEC50 = 4 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.02.012
8593 253 34 None -10 6 Human 4.0 pEC50 = 4 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.02.012
CHEMBL667 253 34 None -10 6 Human 4.0 pEC50 = 4 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.02.012
DB03128 253 34 None -10 6 Human 4.0 pEC50 = 4 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.02.012
163938 106435 13 None -316 2 Human 4.0 pEC50 = 4 Functional
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 180 1 1 5 0.1 Nc1noc(C2CN3CCC2C3)n1 10.1016/S0960-894X(00)80538-7
CHEMBL314737 106435 13 None -316 2 Human 4.0 pEC50 = 4 Functional
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 180 1 1 5 0.1 Nc1noc(C2CN3CCC2C3)n1 10.1016/S0960-894X(00)80538-7
117973690 136473 0 None - 1 Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 5 2 6 3.3 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
CHEMBL3745973 136473 0 None - 1 Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 5 2 6 3.3 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
20918653 115949 5 None - 1 Human 6.0 pEC50 = 6 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 383 4 0 4 4.5 O=c1c2cn(Cc3ccccc3)c3ccccc3c-2nn1Cc1ccccc1F 10.1016/j.bmcl.2014.11.011
CHEMBL3360928 115949 5 None - 1 Human 6.0 pEC50 = 6 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 383 4 0 4 4.5 O=c1c2cn(Cc3ccccc3)c3ccccc3c-2nn1Cc1ccccc1F 10.1016/j.bmcl.2014.11.011
15860348 117957 0 None -4 2 Human 7.0 pEC50 = 7.0 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 283 6 0 6 2.2 CCCCOc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
CHEMBL341242 117957 0 None -4 2 Human 7.0 pEC50 = 7.0 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 283 6 0 6 2.2 CCCCOc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
162659967 180680 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 434 5 2 6 2.7 Cc1c(Cc2ccc(-c3ccn(C)n3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
CHEMBL4761922 180680 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 434 5 2 6 2.7 Cc1c(Cc2ccc(-c3ccn(C)n3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
146216751 184741 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cc2cc(-c3cc(F)c(CN4Cc5sccc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4859577 184741 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cc2cc(-c3cc(F)c(CN4Cc5sccc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
124415421 164101 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 300 1 1 2 4.3 C[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4216615 164101 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 300 1 1 2 4.3 C[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
44579375 192627 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 438 4 1 4 4.6 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL523657 192627 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 438 4 1 4 4.6 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
44251558 7143 0 None 1 2 Rat 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2cc(F)c(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1 nan
CHEMBL1085686 7143 0 None 1 2 Rat 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2cc(F)c(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1 nan
139414093 162992 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 342 3 1 2 5.5 CCC[C@]1(C)N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4202915 162992 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 342 3 1 2 5.5 CCC[C@]1(C)N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
122190997 123089 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 493 5 3 4 5.0 COc1ccc(N/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618439 123089 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 493 5 3 4 5.0 COc1ccc(N/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
117973690 136473 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 415 5 2 6 3.3 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
CHEMBL3745973 136473 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 415 5 2 6 3.3 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
44303396 199551 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 359 3 0 5 3.1 Clc1ccc(C#CCSc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
CHEMBL60374 199551 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 359 3 0 5 3.1 Clc1ccc(C#CCSc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
145962939 160789 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 445 4 2 5 3.0 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(Br)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4125749 160789 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 445 4 2 5 3.0 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(Br)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
162475030 179343 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 456 6 2 6 4.0 COc1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nn4cccc34)cc2)cn1 10.1021/acsmedchemlett.1c00118
CHEMBL4746155 179343 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 456 6 2 6 4.0 COc1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nn4cccc34)cc2)cn1 10.1021/acsmedchemlett.1c00118
118663182 164669 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 392 5 2 6 2.0 Cc1cnc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1021/acs.jmedchem.6b00544
CHEMBL4229092 164669 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 392 5 2 6 2.0 Cc1cnc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1021/acs.jmedchem.6b00544
122186859 122460 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 431 5 2 7 2.4 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608419 122460 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 431 5 2 7 2.4 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2)cn1 10.1021/acsmedchemlett.5b00185
62707610 76001 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 404 5 1 4 3.3 O=C1CCc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059306 76001 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 404 5 1 4 3.3 O=C1CCc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
62705509 76018 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 424 5 1 5 2.9 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3c(F)cccc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059324 76018 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 424 5 1 5 2.9 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3c(F)cccc32)CC1 10.1016/j.bmcl.2012.05.048
53303986 73991 0 None 20 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024407 73991 0 None 20 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
44207908 16555 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 357 6 1 4 1.8 O=C(NC1CCN(CCCN2C(=O)COc3ccccc32)CC1)C1CC1 10.1021/jm100697g
CHEMBL1243267 16555 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 357 6 1 4 1.8 O=C(NC1CCN(CCCN2C(=O)COc3ccccc32)CC1)C1CC1 10.1021/jm100697g
57391102 67912 2 None 2 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 373 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3C)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916224 67912 2 None 2 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 373 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3C)C2)CC1 10.1016/j.bmcl.2011.08.084
44209166 59244 0 None -7 2 Rat 7.0 pEC50 = 7.0 Functional
Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by muscarinic acetylcholine receptor M1)Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by muscarinic acetylcholine receptor M1)
ChEMBL 193 1 0 4 1.0 Cc1noc(C2(C)CN3CCC2C3)n1 10.1021/jm00083a016
CHEMBL171721 59244 0 None -7 2 Rat 7.0 pEC50 = 7.0 Functional
Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by muscarinic acetylcholine receptor M1)Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by muscarinic acetylcholine receptor M1)
ChEMBL 193 1 0 4 1.0 Cc1noc(C2(C)CN3CCC2C3)n1 10.1021/jm00083a016
46872059 67914 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 359 4 1 4 2.5 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3)C2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL1916226 67914 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 359 4 1 4 2.5 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3)C2)CC1 10.1016/j.bmcl.2012.10.132
10686494 100072 0 None -14 3 Human 7.0 pEC50 = 7.0 Functional
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1 10.1016/s0960-894x(98)00509-5
CHEMBL291351 100072 0 None -14 3 Human 7.0 pEC50 = 7.0 Functional
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1 10.1016/s0960-894x(98)00509-5
44303408 200261 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 361 3 0 5 2.6 Fc1cc(Cl)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL60777 200261 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 361 3 0 5 2.6 Fc1cc(Cl)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
10686494 100072 0 None -14 3 Human 7.0 pEC50 = 7.0 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1 10.1021/jm9910019
CHEMBL291351 100072 0 None -14 3 Human 7.0 pEC50 = 7.0 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1 10.1021/jm9910019
70685678 73995 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 6 2 4 2.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1C)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024418 73995 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 6 2 4 2.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1C)C2 10.1016/j.bmcl.2012.03.088
46930074 16541 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 393 7 1 5 2.8 O=C(Cc1ccccc1)NC1CCN(CCCn2c(=O)oc3ccccc32)CC1 10.1021/jm100697g
CHEMBL1243139 16541 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 393 7 1 5 2.8 O=C(Cc1ccccc1)NC1CCN(CCCn2c(=O)oc3ccccc32)CC1 10.1021/jm100697g
44578977 189000 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 469 5 1 6 4.2 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3[N+](=O)[O-])CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL514689 189000 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 469 5 1 6 4.2 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3[N+](=O)[O-])CC2)CC1 10.1016/j.bmcl.2008.09.023
44251558 7143 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPotentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2cc(F)c(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1 10.1016/j.bmcl.2010.01.109
CHEMBL1085686 7143 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPotentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2cc(F)c(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1 10.1016/j.bmcl.2010.01.109
44589500 191979 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 506 3 1 4 4.9 O=C(c1ccccc1C(F)(F)F)N1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL521388 191979 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 506 3 1 4 4.9 O=C(c1ccccc1C(F)(F)F)N1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
127038325 136510 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 402 6 1 6 2.1 CN(C)C(=O)CNC(=O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
CHEMBL3746514 136510 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 402 6 1 6 2.1 CN(C)C(=O)CNC(=O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
146216735 185728 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 463 5 0 6 4.1 Cn1cc2c(-c3cc(F)c(CN4Cc5cnn(CC6CCCO6)c5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4874580 185728 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 463 5 0 6 4.1 Cn1cc2c(-c3cc(F)c(CN4Cc5cnn(CC6CCCO6)c5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
118724608 115960 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 459 5 0 6 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-n5cccn5)cc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360950 115960 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 459 5 0 6 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-n5cccn5)cc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
162655325 180149 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 409 5 2 5 2.8 Cc1cc(F)c(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1021/acs.jmedchem.6b00544
CHEMBL4755820 180149 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 409 5 2 5 2.8 Cc1cc(F)c(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1021/acs.jmedchem.6b00544
118724608 115960 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 459 5 0 6 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-n5cccn5)cc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360950 115960 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 459 5 0 6 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-n5cccn5)cc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
126492039 160838 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 418 5 2 6 2.7 O=C(N[C@H]1CCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126348 160838 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 418 5 2 6 2.7 O=C(N[C@H]1CCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
122190995 123088 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 4 2 3 5.2 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)N(C)c1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618437 123088 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 4 2 3 5.2 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)N(C)c1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
62705172 76002 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 405 5 1 5 2.7 O=C1CCc2ncccc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059307 76002 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 405 5 1 5 2.7 O=C1CCc2ncccc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
71719475 87159 0 None 2 2 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human M1 receptor in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M1 receptor in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 397 4 0 4 3.1 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@H](N3C(=O)Cc4ccccc43)C1)C2 10.1021/ml300372f
CHEMBL2336059 87159 0 None 2 2 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human M1 receptor in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M1 receptor in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 397 4 0 4 3.1 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@H](N3C(=O)Cc4ccccc43)C1)C2 10.1021/ml300372f
145969354 164633 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 422 5 4 6 1.5 Cc1[nH]c(=O)c(C(=O)N[C@H]2CC(O)CC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1016/j.bmcl.2018.04.054
CHEMBL4228557 164633 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 422 5 4 6 1.5 Cc1[nH]c(=O)c(C(=O)N[C@H]2CC(O)CC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1016/j.bmcl.2018.04.054
46890977 6654 0 None 19 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2ccccc2C(=O)NCC2CCNCC2)cc1Cl 10.1016/j.bmcl.2010.04.128
CHEMBL1083723 6654 0 None 19 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2ccccc2C(=O)NCC2CCNCC2)cc1Cl 10.1016/j.bmcl.2010.04.128
42598359 15930 0 None 100 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223864 15930 0 None 100 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
44253016 80047 2 None 1 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
CHEMBL2146597 80047 2 None 1 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
46930073 16538 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 435 8 1 4 3.2 COc1ccc2c(c1)N(CCCN1CCC(NC(=O)Cc3ccccc3)CC1)C(=O)CC2 10.1021/jm100697g
CHEMBL1243109 16538 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 435 8 1 4 3.2 COc1ccc2c(c1)N(CCCN1CCC(NC(=O)Cc3ccccc3)CC1)C(=O)CC2 10.1021/jm100697g
44578976 181398 0 None 9 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 435 5 1 6 3.5 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3[N+](=O)[O-])CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL478034 181398 0 None 9 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 435 5 1 6 3.5 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3[N+](=O)[O-])CC2)CC1 10.1016/j.bmcl.2008.09.023
11734822 116135 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 550 14 0 10 6.4 CN1CCC=C(c2nsnc2SCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL336933 116135 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 550 14 0 10 6.4 CN1CCC=C(c2nsnc2SCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
145985917 164947 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4240517 164947 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
62705331 76008 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 407 5 1 6 2.2 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3ccncc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059314 76008 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 407 5 1 6 2.2 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3ccncc32)CC1 10.1016/j.bmcl.2012.05.048
70685670 73962 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 5 1 4 2.4 CCOC(=O)N1CC[C@H]2[C@H](CCCN2CCNC(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.03.088
CHEMBL2024328 73962 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 5 1 4 2.4 CCOC(=O)N1CC[C@H]2[C@H](CCCN2CCNC(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.03.088
70685676 73987 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 371 4 1 4 2.6 CCOC(=O)N1C2CCC1CC(N1CC[C@H](NC(=O)c3ccccc3)C1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024403 73987 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 371 4 1 4 2.6 CCOC(=O)N1C2CCC1CC(N1CC[C@H](NC(=O)c3ccccc3)C1)C2 10.1016/j.bmcl.2012.03.088
53385831 73988 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 385 4 1 4 3.0 CCOC(=O)N1C2CCC1CC(N1CC[C@@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024404 73988 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 385 4 1 4 3.0 CCOC(=O)N1C2CCC1CC(N1CC[C@@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
53303986 73992 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024408 73992 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
145962939 160789 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 445 4 2 5 3.0 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(Br)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4125749 160789 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 445 4 2 5 3.0 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(Br)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
126492039 160838 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 418 5 2 6 2.7 O=C(N[C@H]1CCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126348 160838 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 418 5 2 6 2.7 O=C(N[C@H]1CCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
44251559 6982 0 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPotentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4c(F)ccc(F)c43)c(F)c2)cn1 10.1016/j.bmcl.2010.01.109
CHEMBL1084940 6982 0 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPotentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4c(F)ccc(F)c43)c(F)c2)cn1 10.1016/j.bmcl.2010.01.109
44303424 198803 0 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 376 3 0 4 4.6 Clc1cc(Cl)cc(C#CCOc2nsnc2C23CC4CC2C3C4)c1 10.1021/jm9910019
CHEMBL59862 198803 0 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 376 3 0 4 4.6 Clc1cc(Cl)cc(C#CCOc2nsnc2C23CC4CC2C3C4)c1 10.1021/jm9910019
145983485 164929 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
CHEMBL4240041 164929 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
145983485 164929 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
CHEMBL4240041 164929 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
145985917 164947 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4240517 164947 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
44251559 6982 0 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4c(F)ccc(F)c43)c(F)c2)cn1 nan
CHEMBL1084940 6982 0 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4c(F)ccc(F)c43)c(F)c2)cn1 nan
145961455 160842 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1nccc1-c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1 10.1016/j.bmcl.2018.05.009
CHEMBL4126400 160842 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1nccc1-c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1 10.1016/j.bmcl.2018.05.009
71540044 85931 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 336 3 1 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(N)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313530 85931 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 336 3 1 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(N)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
1476756 200304 62 None - 1 Human 6.9 pEC50 = 6.9 Functional
Allosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assayAllosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assay
ChEMBL 309 4 1 4 2.8 COc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1 10.1021/jm400540b
CHEMBL608112 200304 62 None - 1 Human 6.9 pEC50 = 6.9 Functional
Allosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assayAllosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assay
ChEMBL 309 4 1 4 2.8 COc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1 10.1021/jm400540b
44208359 16526 0 None 23 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC 10.1021/jm100697g
CHEMBL1242979 16526 0 None 23 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC 10.1021/jm100697g
145984808 165231 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 446 5 2 8 1.8 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4247625 165231 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 446 5 2 8 1.8 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
122186859 122460 0 None -1 2 Rat 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 431 5 2 7 2.4 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608419 122460 0 None -1 2 Rat 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 431 5 2 7 2.4 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2)cn1 10.1021/acsmedchemlett.5b00185
44206730 16528 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 437 8 1 5 2.6 COc1cccc(CC(=O)NC2CCN(CCCN3C(=O)COc4ccccc43)CC2)c1 10.1021/jm100697g
CHEMBL1243010 16528 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 437 8 1 5 2.6 COc1cccc(CC(=O)NC2CCN(CCCN3C(=O)COc4ccccc43)CC2)c1 10.1021/jm100697g
46872059 67914 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 359 4 1 4 2.5 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916226 67914 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 359 4 1 4 2.5 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3)C2)CC1 10.1016/j.bmcl.2011.08.084
57391102 67912 2 None -2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at human recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 373 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3C)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916224 67912 2 None -2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at human recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 373 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3C)C2)CC1 10.1016/j.bmcl.2011.08.084
46873654 67920 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 365 4 1 5 2.6 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccs3)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916232 67920 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 365 4 1 5 2.6 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccs3)C2)CC1 10.1016/j.bmcl.2011.08.084
57391102 67912 2 None 2 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 373 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3C)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916224 67912 2 None 2 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 373 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3C)C2)CC1 10.1016/j.bmcl.2011.08.084
145961455 160842 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1nccc1-c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1 10.1016/j.bmcl.2018.05.009
CHEMBL4126400 160842 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1nccc1-c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1 10.1016/j.bmcl.2018.05.009
71540044 85931 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 336 3 1 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(N)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313530 85931 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 336 3 1 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(N)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
2551 782 23 None -34 12 Human 4.9 pEC50 = 4.9 Functional
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
298 782 23 None -34 12 Human 4.9 pEC50 = 4.9 Functional
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
488 782 23 None -34 12 Human 4.9 pEC50 = 4.9 Functional
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
CHEMBL965 782 23 None -34 12 Human 4.9 pEC50 = 4.9 Functional
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
DB00411 782 23 None -34 12 Human 4.9 pEC50 = 4.9 Functional
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
11072401 30562 0 None -12882 2 Human 4.9 pEC50 = 4.9 Functional
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 592 17 0 10 7.6 CN1CCC=C(c2nsnc2SCCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL139603 30562 0 None -12882 2 Human 4.9 pEC50 = 4.9 Functional
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 592 17 0 10 7.6 CN1CCC=C(c2nsnc2SCCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
72945087 120030 1 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assayAgonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assay
ChEMBL 429 3 0 5 2.8 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(C(=O)N(C)C)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.085
CHEMBL3310802 120030 1 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assayAgonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assay
ChEMBL 429 3 0 5 2.8 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(C(=O)N(C)C)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.085
CHEMBL3545481 120030 1 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assayAgonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assay
ChEMBL 429 3 0 5 2.8 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(C(=O)N(C)C)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.085
162475025 180898 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 426 5 2 5 4.0 O=C(N[C@@H]1CCCC[C@H]1O)c1cc(Cc2ccc(-c3ccncc3)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
CHEMBL4764644 180898 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 426 5 2 5 4.0 O=C(N[C@@H]1CCCC[C@H]1O)c1cc(Cc2ccc(-c3ccncc3)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
3652 4034 72 None -21 9 Human 6.9 pEC50 = 6.9 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
57 4034 72 None -21 9 Human 6.9 pEC50 = 6.9 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
60809 4034 72 None -21 9 Human 6.9 pEC50 = 6.9 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
CHEMBL21536 4034 72 None -21 9 Human 6.9 pEC50 = 6.9 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
DB15357 4034 72 None -21 9 Human 6.9 pEC50 = 6.9 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
10403330 17147 3 None -61 2 Human 6.9 pEC50 = 6.9 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 313 7 0 6 3.3 CCCCCSc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
CHEMBL125732 17147 3 None -61 2 Human 6.9 pEC50 = 6.9 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 313 7 0 6 3.3 CCCCCSc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
44475955 2529 12 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F 10.1016/j.bmcl.2010.12.015
5437 2529 12 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F 10.1016/j.bmcl.2010.12.015
CHEMBL1357815 2529 12 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F 10.1016/j.bmcl.2010.12.015
122195090 123578 0 None 6 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 412 4 1 4 3.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@@H](N3Cc4ccccc4NC3=O)C1)C2 10.1016/j.bmcl.2015.09.032
CHEMBL3633184 123578 0 None 6 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 412 4 1 4 3.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@@H](N3Cc4ccccc4NC3=O)C1)C2 10.1016/j.bmcl.2015.09.032
145984808 165231 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 446 5 2 8 1.8 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4247625 165231 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 446 5 2 8 1.8 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
135409468 2004 63 None 3 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
333 2004 63 None 3 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
CHEMBL845 2004 63 None 3 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
57398164 67915 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 377 4 1 4 2.6 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(F)c3)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916227 67915 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 377 4 1 4 2.6 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(F)c3)C2)CC1 10.1016/j.bmcl.2011.08.084
145961400 161103 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cccc(F)c2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130291 161103 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cccc(F)c2O1 10.1016/j.bmcl.2018.05.009
44589503 185936 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 440 4 1 5 2.8 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL487762 185936 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 440 4 1 5 2.8 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
145963674 161022 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 430 5 2 5 3.5 O=C(N[C@H]1CCCC[C@@H]1O)C1Cc2ccccc2N(Cc2ccc(-n3cccn3)cc2)C1 10.1016/j.bmcl.2018.05.009
CHEMBL4129005 161022 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 430 5 2 5 3.5 O=C(N[C@H]1CCCC[C@@H]1O)C1Cc2ccccc2N(Cc2ccc(-n3cccn3)cc2)C1 10.1016/j.bmcl.2018.05.009
145961400 161103 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cccc(F)c2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130291 161103 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cccc(F)c2O1 10.1016/j.bmcl.2018.05.009
118724597 115953 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccc(F)c4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360939 115953 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccc(F)c4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
118724597 115953 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccc(F)c4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360939 115953 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccc(F)c4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
44475955 2529 12 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F nan
5437 2529 12 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F nan
CHEMBL1357815 2529 12 None -1 2 Rat 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F nan
118663129 182181 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 393 5 2 6 2.5 Cc1cnc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-c2cocn2)cc1 10.1021/acs.jmedchem.6b00544
CHEMBL4790220 182181 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 393 5 2 6 2.5 Cc1cnc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-c2cocn2)cc1 10.1021/acs.jmedchem.6b00544
151866896 182015 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 451 5 2 6 3.9 N#Cc1cncc(-c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)nn4cccc34)cc2)c1 10.1021/acsmedchemlett.1c00118
CHEMBL4788148 182015 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 451 5 2 6 3.9 N#Cc1cncc(-c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)nn4cccc34)cc2)c1 10.1021/acsmedchemlett.1c00118
139414034 163253 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 380 2 1 2 5.8 Fc1ccccc1C1=N[C@@H](c2ccccc2)C(=S)Nc2ccc(Cl)cc21 10.1016/j.bmcl.2017.11.008
CHEMBL4206098 163253 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 380 2 1 2 5.8 Fc1ccccc1C1=N[C@@H](c2ccccc2)C(=S)Nc2ccc(Cl)cc21 10.1016/j.bmcl.2017.11.008
139414036 164194 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 370 3 1 2 6.0 CC(C)[C@@H]1N=C(c2ccccc2)c2cc(-c3ccccc3)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4217684 164194 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 370 3 1 2 6.0 CC(C)[C@@H]1N=C(c2ccccc2)c2cc(-c3ccccc3)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
162475031 180493 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 444 5 2 5 4.2 O=C(N[C@@H]1CCCC[C@H]1O)c1cc(Cc2ccc(-c3ccc(F)cn3)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
CHEMBL4759834 180493 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 444 5 2 5 4.2 O=C(N[C@@H]1CCCC[C@H]1O)c1cc(Cc2ccc(-c3ccc(F)cn3)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
44208564 16524 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 441 7 1 3 3.5 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
CHEMBL1242951 16524 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 441 7 1 3 3.5 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
118732897 120358 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 621 12 1 6 4.9 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Br)ccc2c1=O 10.1021/jm500860w
CHEMBL3414842 120358 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 621 12 1 6 4.9 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Br)ccc2c1=O 10.1021/jm500860w
CHEMBL3559129 120358 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 621 12 1 6 4.9 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Br)ccc2c1=O 10.1021/jm500860w
122186861 122462 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2F)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608421 122462 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2F)cn1 10.1021/acsmedchemlett.5b00185
10426487 2798 4 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 10.1016/s0960-894x(98)00509-5
291 2798 4 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 10.1016/s0960-894x(98)00509-5
CHEMBL99521 2798 4 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 10.1016/s0960-894x(98)00509-5
46891595 6410 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1082680 6410 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
289 240 6 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
9948320 240 6 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
CHEMBL1242950 240 6 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
46929965 16529 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 423 7 1 3 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3c(F)cccc32)CC1 10.1021/jm100697g
CHEMBL1243011 16529 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 423 7 1 3 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3c(F)cccc32)CC1 10.1021/jm100697g
70681453 74002 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 4 2.4 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)C1CCCCC1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024426 74002 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 4 2.4 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)C1CCCCC1)C2 10.1016/j.bmcl.2012.03.088
44578928 190480 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 492 4 1 4 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL518747 190480 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 492 4 1 4 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
10952416 34924 0 None -323 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 578 16 0 10 7.2 CN1CCC=C(c2nsnc2SCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143466 34924 0 None -323 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 578 16 0 10 7.2 CN1CCC=C(c2nsnc2SCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
146216732 184959 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 423 5 1 6 2.9 Cn1cc2c(-c3cc(F)c(CN4Cc5cnn(CCO)c5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4862985 184959 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 423 5 1 6 2.9 Cn1cc2c(-c3cc(F)c(CN4Cc5cnn(CCO)c5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
122191005 123097 0 None 3 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 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 123097 0 None 3 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 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
118724604 115957 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccncc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360946 115957 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccncc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
118724604 115957 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccncc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360946 115957 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccncc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
3652 4034 72 None -21 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4034 72 None -21 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4034 72 None -21 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4034 72 None -21 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4034 72 None -21 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
3652 4034 72 None -21 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4034 72 None -21 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4034 72 None -21 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4034 72 None -21 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4034 72 None -21 9 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
46891142 6485 0 None 63 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 364 4 2 2 3.8 O=C(NC[C@H]1CCNC[C@H]1F)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083003 6485 0 None 63 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 364 4 2 2 3.8 O=C(NC[C@H]1CCNC[C@H]1F)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46891143 6558 0 None 63 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 396 4 2 2 4.7 O=C(NCC1=C(F)CNCC1)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
CHEMBL1083317 6558 0 None 63 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 396 4 2 2 4.7 O=C(NCC1=C(F)CNCC1)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
46891031 6590 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(Cl)cc1-c1ccccc1C(=O)NCC1CCNCC1 10.1016/j.bmcl.2010.04.128
CHEMBL1083419 6590 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(Cl)cc1-c1ccccc1C(=O)NCC1CCNCC1 10.1016/j.bmcl.2010.04.128
46890717 6651 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(C(=O)NCC2CCNCC2)c(-c2cccc(Cl)c2)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083717 6651 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(C(=O)NCC2CCNCC2)c(-c2cccc(Cl)c2)c1 10.1016/j.bmcl.2010.04.127
46891077 6736 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 392 4 2 2 4.7 CC1CNCC=C1CNC(=O)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
CHEMBL1083927 6736 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 392 4 2 2 4.7 CC1CNCC=C1CNC(=O)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
46890962 6942 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 328 4 2 2 3.4 O=C(Cc1ccccc1-c1cccc(Cl)c1)NC1CCNCC1 10.1016/j.bmcl.2010.04.127
CHEMBL1084804 6942 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 328 4 2 2 3.4 O=C(Cc1ccccc1-c1cccc(Cl)c1)NC1CCNCC1 10.1016/j.bmcl.2010.04.127
145986042 165325 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 6 1 7 3.1 Cn1ccc(-c2ccc(Cc3cc(C(=O)NCC4CCOCC4)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4249357 165325 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 6 1 7 3.1 Cn1ccc(-c2ccc(Cc3cc(C(=O)NCC4CCOCC4)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
46891029 6516 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1cc(Cl)cc(-c2ccccc2C(=O)NCC2CCNCC2)c1 10.1016/j.bmcl.2010.04.128
CHEMBL1083107 6516 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1cc(Cl)cc(-c2ccccc2C(=O)NCC2CCNCC2)c1 10.1016/j.bmcl.2010.04.128
46891019 6581 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 410 6 1 3 3.9 CS(=O)(=O)N(Cc1c(F)cccc1-c1cccc(Cl)c1)CC1CCNCC1 10.1016/j.bmcl.2010.04.127
CHEMBL1083401 6581 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 410 6 1 3 3.9 CS(=O)(=O)N(Cc1c(F)cccc1-c1cccc(Cl)c1)CC1CCNCC1 10.1016/j.bmcl.2010.04.127
145986042 165325 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 6 1 7 3.1 Cn1ccc(-c2ccc(Cc3cc(C(=O)NCC4CCOCC4)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4249357 165325 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 6 1 7 3.1 Cn1ccc(-c2ccc(Cc3cc(C(=O)NCC4CCOCC4)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
2551 782 23 None -34 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 782 23 None -34 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 782 23 None -34 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 782 23 None -34 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 782 23 None -34 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
2551 782 23 None -34 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 782 23 None -34 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 782 23 None -34 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 782 23 None -34 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 782 23 None -34 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
49799920 10442 0 None 6 2 Human 6.8 pEC50 = 6.8 Functional
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 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 10442 0 None 6 2 Human 6.8 pEC50 = 6.8 Functional
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CC[C@@H]1C2 10.1016/s0960-894x(98)00509-5
145969659 164408 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 431 5 3 7 2.3 O=C(N[C@H]1CCC(O)C[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
CHEMBL4225188 164408 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 431 5 3 7 2.3 O=C(N[C@H]1CCC(O)C[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
44215433 76000 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 387 5 1 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(c2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059305 76000 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 387 5 1 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(c2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2012.05.048
46930252 16557 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 371 6 1 4 2.2 O=C(NC1CCN(CCCN2C(=O)COc3ccccc32)CC1)C1CCC1 10.1021/jm100697g
CHEMBL1243295 16557 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 371 6 1 4 2.2 O=C(NC1CCN(CCCN2C(=O)COc3ccccc32)CC1)C1CCC1 10.1021/jm100697g
25010776 55664 1 None 1 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2012.03.088
CHEMBL1559151 55664 1 None 1 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2012.03.088
CHEMBL1624037 55664 1 None 1 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2012.03.088
44579416 186479 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 449 4 1 5 4.2 N#Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL491208 186479 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 449 4 1 5 4.2 N#Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
118124140 160868 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2F)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126807 160868 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2F)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
22730942 17922 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 271 5 0 6 2.1 CCCSc1nsnc1OC1CN2CCC1C2 10.1021/jm970125n
CHEMBL126846 17922 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 271 5 0 6 2.1 CCCSc1nsnc1OC1CN2CCC1C2 10.1021/jm970125n
145969333 164608 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 425 5 3 7 2.3 Cc1cnc(C(=O)N[C@H]2CCOC(O)[C@@H]2O)cc1Cc1ccc(-c2cscn2)cc1 10.1016/j.bmcl.2018.04.054
CHEMBL4228097 164608 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 425 5 3 7 2.3 Cc1cnc(C(=O)N[C@H]2CCOC(O)[C@@H]2O)cc1Cc1ccc(-c2cscn2)cc1 10.1016/j.bmcl.2018.04.054
122186858 122459 0 None -2 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 405 4 2 7 1.9 Cn1ncc2cc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)ccc21 10.1021/acsmedchemlett.5b00185
CHEMBL3608418 122459 0 None -2 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 405 4 2 7 1.9 Cn1ncc2cc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)ccc21 10.1021/acsmedchemlett.5b00185
126492034 160874 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 441 6 1 7 3.7 COc1cccnc1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126841 160874 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 441 6 1 7 3.7 COc1cccnc1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
127039038 136515 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 414 5 2 5 3.9 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2ccccc12 10.1016/j.bmcl.2015.11.053
CHEMBL3746599 136515 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 414 5 2 5 3.9 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2ccccc12 10.1016/j.bmcl.2015.11.053
9904307 19263 0 None -6 2 Human 6.8 pEC50 = 6.8 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 297 7 0 6 2.6 CCCCCOc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
CHEMBL129764 19263 0 None -6 2 Human 6.8 pEC50 = 6.8 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 297 7 0 6 2.6 CCCCCOc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
145964557 163667 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 2 1 2 4.8 Fc1ccccc1C1=N[C@@H](C2CC2)C(=S)Nc2ccc(Cl)cc21 10.1016/j.bmcl.2017.11.008
CHEMBL4211028 163667 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 2 1 2 4.8 Fc1ccccc1C1=N[C@@H](C2CC2)C(=S)Nc2ccc(Cl)cc21 10.1016/j.bmcl.2017.11.008
122189494 122818 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 461 6 2 4 4.4 COc1ccc(C(=O)N[C@@H]2c3cc(/N=C(\C)N(C)Cc4ccc(F)cc4)ccc3C[C@H]2O)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3616498 122818 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 461 6 2 4 4.4 COc1ccc(C(=O)N[C@@H]2c3cc(/N=C(\C)N(C)Cc4ccc(F)cc4)ccc3C[C@H]2O)cc1 10.1016/j.bmcl.2015.08.011
162648092 179311 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 437 5 2 6 3.4 Cc1c(Cc2ccc(-c3cscn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
CHEMBL4745827 179311 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 437 5 2 6 3.4 Cc1c(Cc2ccc(-c3cscn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
146216707 183876 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 463 5 0 6 4.1 Cn1cc2cc(-c3cc(F)c(CN4Cc5cnn(CC6CCCO6)c5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4846688 183876 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 463 5 0 6 4.1 Cn1cc2cc(-c3cc(F)c(CN4Cc5cnn(CC6CCCO6)c5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
145969659 164408 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 431 5 3 7 2.3 O=C(N[C@H]1CCC(O)C[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
CHEMBL4225188 164408 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 431 5 3 7 2.3 O=C(N[C@H]1CCC(O)C[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
162658825 180418 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 453 6 2 6 2.5 CO[C@@H]1CCN(c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)c(=O)n(C)c3C)cc2)C1 10.1021/acs.jmedchem.6b00544
CHEMBL4758929 180418 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 453 6 2 6 2.5 CO[C@@H]1CCN(c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)c(=O)n(C)c3C)cc2)C1 10.1021/acs.jmedchem.6b00544
127049133 140503 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 393 3 0 4 3.7 Cn1cc2c(-c3cc(F)c(CN4C=CC5=NCCN5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
CHEMBL3823999 140503 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 393 3 0 4 3.7 Cn1cc2c(-c3cc(F)c(CN4C=CC5=NCCN5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
53385782 73964 0 None 56 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 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 73964 0 None 56 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 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
2166 3074 46 None -25 8 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/j.bmcl.2015.02.012
305 3074 46 None -25 8 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/j.bmcl.2015.02.012
5910 3074 46 None -25 8 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/j.bmcl.2015.02.012
CHEMBL550 3074 46 None -25 8 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/j.bmcl.2015.02.012
DB01085 3074 46 None -25 8 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/j.bmcl.2015.02.012
76335135 102791 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 6 2 4 2.2 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1C 10.1016/j.bmcl.2012.03.088
CHEMBL3084448 102791 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 6 2 4 2.2 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1C 10.1016/j.bmcl.2012.03.088
76331523 102798 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 5 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccs1 10.1016/j.bmcl.2012.03.088
CHEMBL3084456 102798 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 5 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccs1 10.1016/j.bmcl.2012.03.088
62705330 76007 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 407 5 1 6 2.2 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3cccnc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059313 76007 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 407 5 1 6 2.2 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3cccnc32)CC1 10.1016/j.bmcl.2012.05.048
127050528 140458 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 393 3 0 5 3.4 Cn1cc2cc(-c3cc(F)c(CN4CCn5nccc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2016.04.083
CHEMBL3823424 140458 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 393 3 0 5 3.4 Cn1cc2cc(-c3cc(F)c(CN4CCn5nccc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2016.04.083
127049133 140503 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 393 3 0 4 3.7 Cn1cc2c(-c3cc(F)c(CN4C=CC5=NCCN5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
CHEMBL3823999 140503 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 393 3 0 4 3.7 Cn1cc2c(-c3cc(F)c(CN4C=CC5=NCCN5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
126492034 160874 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 441 6 1 7 3.7 COc1cccnc1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126841 160874 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 441 6 1 7 3.7 COc1cccnc1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
139414122 163759 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 362 2 1 2 5.6 CC(C)[C@@H]1N=C(c2cccc(Cl)c2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4212268 163759 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 362 2 1 2 5.6 CC(C)[C@@H]1N=C(c2cccc(Cl)c2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
118729455 117347 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 182 1 1 4 0.3 CN1CCC=C(C2=NOC(O)C2)C1 10.1016/j.bmcl.2015.02.012
CHEMBL3402922 117347 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 182 1 1 4 0.3 CN1CCC=C(C2=NOC(O)C2)C1 10.1016/j.bmcl.2015.02.012
145982858 165246 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 432 5 1 6 4.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)NC3CCOCC3)nc21 10.1021/acsmedchemlett.8b00261
CHEMBL4248069 165246 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 432 5 1 6 4.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)NC3CCOCC3)nc21 10.1021/acsmedchemlett.8b00261
145982858 165246 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 432 5 1 6 4.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)NC3CCOCC3)nc21 10.1021/acsmedchemlett.8b00261
CHEMBL4248069 165246 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 432 5 1 6 4.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)NC3CCOCC3)nc21 10.1021/acsmedchemlett.8b00261
127042157 136565 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 401 6 1 6 3.2 O=C(NC[C@@H]1CCCO1)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
CHEMBL3747254 136565 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 401 6 1 6 3.2 O=C(NC[C@@H]1CCCO1)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
145986351 164675 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 452 6 4 8 0.7 Cn1c(CO)c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCC(O)C[C@@H]2O)c1=O 10.1016/j.bmcl.2018.04.054
CHEMBL4229133 164675 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 452 6 4 8 0.7 Cn1c(CO)c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCC(O)C[C@@H]2O)c1=O 10.1016/j.bmcl.2018.04.054
118732895 120357 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 561 12 1 6 4.3 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2c(F)cccc2c1=O 10.1021/jm500860w
CHEMBL3414841 120357 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 561 12 1 6 4.3 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2c(F)cccc2c1=O 10.1021/jm500860w
CHEMBL3559128 120357 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 561 12 1 6 4.3 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2c(F)cccc2c1=O 10.1021/jm500860w
145962181 160950 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1cc(-c2ccc(CN3CC(C(=O)N[C@H]4CCCC[C@@H]4O)Oc4ccccc43)cn2)cn1 10.1016/j.bmcl.2018.05.009
CHEMBL4128022 160950 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1cc(-c2ccc(CN3CC(C(=O)N[C@H]4CCCC[C@@H]4O)Oc4ccccc43)cn2)cn1 10.1016/j.bmcl.2018.05.009
76313419 102790 0 None 69 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1 10.1016/j.bmcl.2012.03.088
CHEMBL3084447 102790 0 None 69 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1 10.1016/j.bmcl.2012.03.088
135409468 2004 63 None 3 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
333 2004 63 None 3 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
CHEMBL845 2004 63 None 3 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
122186861 122462 0 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2F)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608421 122462 0 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2F)cn1 10.1021/acsmedchemlett.5b00185
122186862 122463 0 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 408 5 3 6 1.3 CNC(=O)c1ccc(Cn2cc(C(=O)N[C@H]3COCC[C@@H]3O)c3ncccc32)cc1 10.1021/acsmedchemlett.5b00185
CHEMBL3608422 122463 0 None -1 2 Rat 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 408 5 3 6 1.3 CNC(=O)c1ccc(Cn2cc(C(=O)N[C@H]3COCC[C@@H]3O)c3ncccc32)cc1 10.1021/acsmedchemlett.5b00185
44207907 16548 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 331 5 1 4 1.4 CC(=O)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
CHEMBL1243202 16548 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 331 5 1 4 1.4 CC(=O)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
11124824 32031 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 522 12 0 10 5.7 CN1CCC=C(c2nsnc2SCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL140985 32031 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 522 12 0 10 5.7 CN1CCC=C(c2nsnc2SCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
145985065 165177 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4246159 165177 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
826706 41505 64 None 70 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 286 1 1 2 4.2 SC1=Nc2ccc(Cl)cc2C(c2ccccc2)=NC1 10.1016/j.bmcl.2017.11.008
CHEMBL1492697 41505 64 None 70 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 286 1 1 2 4.2 SC1=Nc2ccc(Cl)cc2C(c2ccccc2)=NC1 10.1016/j.bmcl.2017.11.008
145985065 165177 0 None -2 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4246159 165177 0 None -2 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
44578975 189111 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 4 4.9 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL515489 189111 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 4 4.9 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2008.09.023
146487745 180250 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 413 5 1 4 3.6 O=C(NCC1CCCO1)c1cc(Cc2ccc(Br)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
CHEMBL4756974 180250 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 413 5 1 4 3.6 O=C(NCC1CCCO1)c1cc(Cc2ccc(Br)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
145985065 165177 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4246159 165177 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
145985065 165177 0 None -2 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4246159 165177 0 None -2 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
44303293 199741 0 None -3 3 Human 5.7 pEC50 = 5.7 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 393 3 0 5 3.8 Clc1cc(Cl)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL60479 199741 0 None -3 3 Human 5.7 pEC50 = 5.7 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 393 3 0 5 3.8 Clc1cc(Cl)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
146487799 181660 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 415 5 1 6 3.2 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nn4cccc34)cc2)cn1 10.1021/acsmedchemlett.1c00118
CHEMBL4783540 181660 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 415 5 1 6 3.2 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nn4cccc34)cc2)cn1 10.1021/acsmedchemlett.1c00118
122191003 123096 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 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 123096 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 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
145970842 164455 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 459 6 2 8 2.2 Cn1ccc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@H]4O)c4nc(C=O)ccc43)cc2)n1 10.1016/j.bmcl.2018.04.054
CHEMBL4225919 164455 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 459 6 2 8 2.2 Cn1ccc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@H]4O)c4nc(C=O)ccc43)cc2)n1 10.1016/j.bmcl.2018.04.054
139414055 163726 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 2 2 3 4.1 CC(C)(O)C1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4211802 163726 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 2 2 3 4.1 CC(C)(O)C1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
127038317 136540 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 400 4 2 5 3.7 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc3ncccc3c2)c2cccnc12 10.1016/j.bmcl.2015.11.053
CHEMBL3746904 136540 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 400 4 2 5 3.7 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc3ncccc3c2)c2cccnc12 10.1016/j.bmcl.2015.11.053
44475948 61460 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 511 7 2 7 4.1 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cn[nH]c4)c3)c3cc(F)cc(F)c23)no1 10.1016/j.bmcl.2010.12.015
CHEMBL1773111 61460 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 511 7 2 7 4.1 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cn[nH]c4)c3)c3cc(F)cc(F)c23)no1 10.1016/j.bmcl.2010.12.015
145963718 161090 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 434 5 2 7 1.9 O=C(N[C@H]1CCOC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130084 161090 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 434 5 2 7 1.9 O=C(N[C@H]1CCOC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
139414015 163023 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 314 2 1 2 4.7 CC[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4203218 163023 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 314 2 1 2 4.7 CC[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
44207904 16562 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 361 6 1 3 2.5 CCC(=O)NC1CCN(CCCN2C(=O)CCc3c(F)cccc32)CC1 10.1021/jm100697g
CHEMBL1243328 16562 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 361 6 1 3 2.5 CCC(=O)NC1CCN(CCCN2C(=O)CCc3c(F)cccc32)CC1 10.1021/jm100697g
46891075 6735 0 None 125 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083926 6735 0 None 125 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46871666 6991 0 None 63 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 CC1CNCCC1CNC(=O)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
CHEMBL1084993 6991 0 None 63 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 CC1CNCCC1CNC(=O)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
145963718 161090 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 434 5 2 7 1.9 O=C(N[C@H]1CCOC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130084 161090 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 434 5 2 7 1.9 O=C(N[C@H]1CCOC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
70689865 73999 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 381 6 2 4 2.4 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cc(F)cc(F)c1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024423 73999 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 381 6 2 4 2.4 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cc(F)cc(F)c1)C2 10.1016/j.bmcl.2012.03.088
10397356 120204 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL354738 120204 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
71555066 140433 12 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 322 3 0 4 2.8 Cn1cc(-c2ccc(CN3Cc4ncccc4C3=O)c(F)c2)cn1 10.1016/j.bmcl.2016.04.083
CHEMBL3823130 140433 12 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 322 3 0 4 2.8 Cn1cc(-c2ccc(CN3Cc4ncccc4C3=O)c(F)c2)cn1 10.1016/j.bmcl.2016.04.083
145961193 161101 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 432 7 2 6 2.9 CC(O)(CNC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1)C1CC1 10.1016/j.bmcl.2018.05.009
CHEMBL4130287 161101 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 432 7 2 6 2.9 CC(O)(CNC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1)C1CC1 10.1016/j.bmcl.2018.05.009
145961193 161101 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 432 7 2 6 2.9 CC(O)(CNC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1)C1CC1 10.1016/j.bmcl.2018.05.009
CHEMBL4130287 161101 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 432 7 2 6 2.9 CC(O)(CNC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1)C1CC1 10.1016/j.bmcl.2018.05.009
146216704 185611 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cc2c(-c3cc(F)c(CN4Cc5sccc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4872836 185611 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cc2c(-c3cc(F)c(CN4Cc5sccc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
118724607 115959 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 491 5 0 6 5.6 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-c5cnn(C)c5)cc4F)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360949 115959 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 491 5 0 6 5.6 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-c5cnn(C)c5)cc4F)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
118724607 115959 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 491 5 0 6 5.6 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-c5cnn(C)c5)cc4F)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360949 115959 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 491 5 0 6 5.6 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-c5cnn(C)c5)cc4F)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
122190998 123091 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 3 4 4.7 COc1cccc(CN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)c1 10.1016/j.bmcl.2015.08.011
CHEMBL3618441 123091 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 3 4 4.7 COc1cccc(CN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)c1 10.1016/j.bmcl.2015.08.011
42598586 15947 0 None 1 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223938 15947 0 None 1 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
9913341 81746 3 None -630 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL216927 81746 3 None -630 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL553058 81746 3 None -630 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
10104167 2028 1 None -14 3 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 10.1021/jm500860w
6937 2028 1 None -14 3 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 10.1021/jm500860w
CHEMBL3121473 2028 1 None -14 3 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 10.1021/jm500860w
22745278 186480 1 None 4 5 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 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 186480 1 None 4 5 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 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
129456 205443 11 None -8 2 Rat 8.6 pEC50 = 8.6 Functional
Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by Muscarinic M1 receptor)Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by Muscarinic M1 receptor)
ChEMBL 179 1 0 4 0.8 Cc1noc(C2CN3CCC2C3)n1 10.1021/jm00083a016
CHEMBL92421 205443 11 None -8 2 Rat 8.6 pEC50 = 8.6 Functional
Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by Muscarinic M1 receptor)Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by Muscarinic M1 receptor)
ChEMBL 179 1 0 4 0.8 Cc1noc(C2CN3CCC2C3)n1 10.1021/jm00083a016
44303314 100466 0 None 10 3 Human 8.6 pEC50 = 8.6 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 343 3 0 5 2.6 Fc1cccc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL293982 100466 0 None 10 3 Human 8.6 pEC50 = 8.6 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 343 3 0 5 2.6 Fc1cccc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
42598360 15928 0 None 63 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223862 15928 0 None 63 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42599071 15948 0 None 125 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223939 15948 0 None 125 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25230693 15949 0 None 63 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223940 15949 0 None 63 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
62705175 76004 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 405 5 1 5 2.7 O=C1CCc2cccnc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059310 76004 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 405 5 1 5 2.7 O=C1CCc2cccnc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
46930342 16571 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 361 6 1 3 2.5 CCC(=O)NC1CCN(CCCN2C(=O)CCc3ccc(F)cc32)CC1 10.1021/jm100697g
CHEMBL1243358 16571 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 361 6 1 3 2.5 CCC(=O)NC1CCN(CCCN2C(=O)CCc3ccc(F)cc32)CC1 10.1021/jm100697g
44207447 16577 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 379 6 1 3 2.6 CCC(=O)NC1CCN(CCCN2C(=O)CCc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
CHEMBL1243387 16577 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 379 6 1 3 2.6 CCC(=O)NC1CCN(CCCN2C(=O)CCc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
162646208 178894 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 422 5 2 7 1.4 Cc1c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCOC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
CHEMBL4740865 178894 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 422 5 2 7 1.4 Cc1c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCOC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
11725107 100147 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 345 3 0 5 2.1 Fc1cc(F)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL291872 100147 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 345 3 0 5 2.1 Fc1cc(F)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
59654579 123090 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 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 123090 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 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
76335136 102794 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 381 6 2 4 2.2 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cc(F)cc(F)c1 10.1016/j.bmcl.2012.03.088
CHEMBL3084451 102794 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 381 6 2 4 2.2 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cc(F)cc(F)c1 10.1016/j.bmcl.2012.03.088
25010776 55664 1 None -1 5 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1559151 55664 1 None -1 5 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1624037 55664 1 None -1 5 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2011.08.084
3652 4034 72 None -21 9 Human 6.7 pEC50 = 6.7 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm970125n
57 4034 72 None -21 9 Human 6.7 pEC50 = 6.7 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm970125n
60809 4034 72 None -21 9 Human 6.7 pEC50 = 6.7 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm970125n
CHEMBL21536 4034 72 None -21 9 Human 6.7 pEC50 = 6.7 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm970125n
DB15357 4034 72 None -21 9 Human 6.7 pEC50 = 6.7 Functional
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm970125n
650899 54129 10 None 4 5 Rat 6.7 pEC50 = 6.7 Functional
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL1535797 54129 10 None 4 5 Rat 6.7 pEC50 = 6.7 Functional
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL1609153 54129 10 None 4 5 Rat 6.7 pEC50 = 6.7 Functional
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.132
71737672 2539 14 None -3 6 Rat 5.7 pEC50 = 5.7 Functional
Activity at rat muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2539 14 None -3 6 Rat 5.7 pEC50 = 5.7 Functional
Activity at rat muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2539 14 None -3 6 Rat 5.7 pEC50 = 5.7 Functional
Activity at rat muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
70687733 73827 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 354 5 2 5 0.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)N1CCOCC1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2022944 73827 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 354 5 2 5 0.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)N1CCOCC1)C2 10.1016/j.bmcl.2012.03.088
70687828 73993 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 357 7 2 4 2.3 C=CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024410 73993 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 357 7 2 4 2.3 C=CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
71717377 86137 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 437 4 1 4 3.3 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(Br)c3)C2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL2315678 86137 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 437 4 1 4 3.3 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(Br)c3)C2)CC1 10.1016/j.bmcl.2012.10.132
146216775 183950 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 378 3 0 5 4.0 Cn1cc2cc(-c3ccc(CN4Cc5ncsc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4847801 183950 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 378 3 0 5 4.0 Cn1cc2cc(-c3ccc(CN4Cc5ncsc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
187 253 34 None -10