Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
9927975 4110 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 4110 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 15864 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 15864 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 15887 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 15887 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 206412 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 206412 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 15886 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 15886 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 115948 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 115948 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 186425 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 186425 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 6719 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 6719 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 192459 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 192459 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 110909 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 110909 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 6949 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 6949 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 15911 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 15911 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 117544 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 117544 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 106710 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 106710 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 186269 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 186269 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 186389 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 186389 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 100058 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 100058 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 100058 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 115949 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 115949 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 15912 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 15912 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 2917 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 2917 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 2917 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 4022 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 4022 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 4022 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 4022 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 4022 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 192074 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 192074 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 198163 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 198163 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 17907 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 17907 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 115486 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 115486 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 6325 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 6325 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 6502 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 6502 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 15935 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 15935 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 16507 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 16507 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 10000 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 10000 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 115950 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 115950 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 200329 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 200329 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 6306 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 6306 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 6524 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 6524 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 16525 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 16525 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 164816 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 164816 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 136031 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 136031 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 73813 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 73813 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 102782 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 102782 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 6637 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 6637 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 6875 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 6875 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 6950 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 6950 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 115936 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 115936 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 106422 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 106422 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 136460 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 136460 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 115936 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 115936 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 117944 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 117944 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 180670 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 180670 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 184731 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 184731 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 164090 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 164090 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 192617 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 192617 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 7128 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 7128 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 162980 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 162980 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 123076 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 123076 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 136460 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 136460 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 199541 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 199541 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 160777 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 160777 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 179333 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 179333 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 164658 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 164658 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 122447 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 122447 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 75986 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 75986 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 76003 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 76003 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 73976 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 73976 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 16540 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 16540 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 67897 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 67897 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 59229 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 59229 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 67899 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 67899 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 100059 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 100059 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 200252 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 200252 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 100059 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 100059 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 73980 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 73980 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 16526 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 16526 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 188990 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 188990 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 7128 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 7128 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 191969 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 191969 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 136497 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 136497 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 185718 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 185718 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 115947 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 115947 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 180139 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 180139 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 115947 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 115947 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 160826 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 160826 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 123075 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 123075 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 75987 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 75987 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 87145 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 87145 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 164622 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 164622 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 6639 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 6639 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 15915 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 15915 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 80032 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 80032 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 16523 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 16523 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 181388 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 181388 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 116122 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 116122 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 164936 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 164936 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 75993 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 75993 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 73947 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 73947 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 73972 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 73972 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 73973 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 73973 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 73977 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 73977 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 160777 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 160777 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 160826 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 160826 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 6967 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 6967 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 198793 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 198793 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 164918 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 164918 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 164918 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 164918 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 164936 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 164936 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 6967 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 6967 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 160830 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 160830 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 85917 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 85917 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 200295 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 200295 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 16511 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 16511 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 165220 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 165220 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 122447 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 122447 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 16513 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 16513 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 67899 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 67899 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 67897 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 67897 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 67905 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 67905 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 67897 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 67897 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 160830 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 160830 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 85917 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 85917 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 780 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
298 780 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
488 780 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 780 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 780 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 30547 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 30547 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 120017 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 120017 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 120017 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 180888 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 180888 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 4022 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 4022 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 4022 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 4022 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 4022 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 17132 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 17132 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 2519 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 2519 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 2519 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 123565 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 123565 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 165220 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 165220 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 1996 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 1996 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 1996 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 67900 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 67900 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 161091 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 161091 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 185926 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 185926 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 161010 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 161010 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 161091 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 161091 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 115940 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 115940 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 115940 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 115940 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 2519 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 2519 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 2519 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 182171 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 182171 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 182005 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 182005 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 163242 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 163242 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 164183 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 164183 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 180483 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 180483 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 16509 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 16509 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 120345 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 120345 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 120345 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 122449 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 122449 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 2788 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 2788 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 2788 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 6395 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 6395 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 16514 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 16514 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 73987 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 73987 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 190470 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 190470 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 34909 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 34909 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 184949 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 184949 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 123084 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 123084 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 115944 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 115944 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 115944 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 115944 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 4022 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 4022 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 4022 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 4022 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 4022 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 4022 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 4022 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 4022 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 4022 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 4022 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 6470 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 6470 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 6543 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 6543 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 6575 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 6575 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 6636 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 6636 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 6721 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 6721 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 6927 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 6927 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 165314 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 165314 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 6501 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 6501 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 6566 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 6566 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 165314 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 165314 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 780 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
298 780 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
488 780 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 780 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 780 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 780 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
298 780 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
488 780 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 780 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 780 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 10427 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 10427 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 164397 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 164397 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 75985 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 75985 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 16542 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 16542 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 55649 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 55649 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 55649 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 186469 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 186469 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 160856 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 160856 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 17907 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 17907 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 164597 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 164597 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 122446 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 122446 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 160862 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 160862 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 136502 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 136502 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 19248 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 19248 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 163656 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 163656 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 122805 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 122805 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 179301 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 179301 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 183866 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 183866 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 164397 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 164397 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 180408 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 180408 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 140490 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 140490 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 73949 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 73949 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 3062 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 3062 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 3062 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 3062 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 3062 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 102778 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 102778 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 102785 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 102785 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 75992 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 75992 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 140445 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 140445 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 140490 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 140490 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 160862 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 160862 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 163748 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 163748 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 117334 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 117334 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 165235 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 165235 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 165235 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 165235 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 136552 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 136552 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 164664 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 164664 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 120344 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 120344 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 120344 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 160938 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 160938 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 102777 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 102777 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 1996 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 1996 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 1996 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 122449 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 122449 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 122450 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 122450 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 16533 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 16533 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 32016 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 32016 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 165166 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 165166 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 41490 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 41490 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 165166 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 165166 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 189101 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 189101 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 180240 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 180240 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 165166 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 165166 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 165166 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 165166 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 199731 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 199731 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 181650 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 181650 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 123083 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 123083 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 164444 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 164444 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 163715 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 163715 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 136527 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 136527 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 61445 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 61445 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 161078 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 161078 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 163011 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 163011 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 16547 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 16547 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 6720 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 6720 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 6976 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 6976 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 161078 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 161078 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 73984 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 73984 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 120191 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 120191 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 140420 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 140420 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 161089 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 161089 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 161089 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 161089 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 185601 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 185601 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 115946 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 115946 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 115946 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 115946 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 123078 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 123078 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 15932 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 15932 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 81732 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 81732 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 81732 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 2020 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 2020 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 2020 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 186470 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 186470 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 205433 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 205433 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 100453 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 100453 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 15913 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 15913 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 15933 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 15933 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 15934 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 15934 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 75989 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 75989 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 16556 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 16556 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 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 379 6 1 3 2.6 CCC(=O)NC1CCN(CCCN2C(=O)CCc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
CHEMBL1243387 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 379 6 1 3 2.6 CCC(=O)NC1CCN(CCCN2C(=O)CCc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
162646208 178884 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 178884 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 100134 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 100134 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 123077 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 123077 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 102781 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 102781 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 55649 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 55649 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 55649 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 4022 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 4022 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 4022 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 4022 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 4022 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 54114 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 54114 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 54114 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 2529 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 2529 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 2529 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 73812 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 73812 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 73978 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 73978 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 86123 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 86123 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 183940 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 183940 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