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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors UniProt IUPHAR Species p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
10104167 1928 0 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 24863257
6937 1928 0 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 24863257
CHEMBL3121473 1928 0 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 24863257
10712 2405 26 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 399 3 1 5 4.3 O[C@H]1CCCC[C@@H]1n1cnc2c(c1=O)cc(c1c2cccc1)Cc1ccc(nc1)C 30034595
46207733 2405 26 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 399 3 1 5 4.3 O[C@H]1CCCC[C@@H]1n1cnc2c(c1=O)cc(c1c2cccc1)Cc1ccc(nc1)C 30034595
CHEMBL4078588 2405 26 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 399 3 1 5 4.3 O[C@H]1CCCC[C@@H]1n1cnc2c(c1=O)cc(c1c2cccc1)Cc1ccc(nc1)C 30034595
DB12897 2405 26 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 399 3 1 5 4.3 O[C@H]1CCCC[C@@H]1n1cnc2c(c1=O)cc(c1c2cccc1)Cc1ccc(nc1)C 30034595
10259 3437 0 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 426 3 0 5 2.8 Cc1cccc(c1)N1CN(C(=O)C21CCN(CC2)C1CCN(CC1)C(=O)OC1CC1)C 30276808
137553163 3437 0 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 426 3 0 5 2.8 Cc1cccc(c1)N1CN(C(=O)C21CCN(CC2)C1CCN(CC1)C(=O)OC1CC1)C 30276808
10711 3502 0 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 406 3 1 4 4.0 O[C@H]1CCC[C@@H]1N1COc2c(C1=O)cc(c(c2Cl)C)Cc1ccc(nc1)Cl 31990455
124155515 3502 0 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 406 3 1 4 4.0 O[C@H]1CCC[C@@H]1N1COc2c(C1=O)cc(c(c2Cl)C)Cc1ccc(nc1)Cl 31990455
135411347 3771 0 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 363 7 3 5 3.5 CCOc1ccc(cc1)NCC(=O)N/N=C/c1c(O)ccc2c1cccc2 19047481
3261 3771 0 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 363 7 3 5 3.5 CCOc1ccc(cc1)NCC(=O)N/N=C/c1c(O)ccc2c1cccc2 19047481
6758210 3771 0 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 363 7 3 5 3.5 CCOc1ccc(cc1)NCC(=O)N/N=C/c1c(O)ccc2c1cccc2 19047481
2882724 3773 0 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 7 2.8 O=C1NC(C(=C(N1C)C)C(=O)OC1CCCC1)c1cc2OCOc2cc1[N+](=O)[O-] 19047481
3259 3773 0 ACM1 M1 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 7 2.8 O=C1NC(C(=C(N1C)C)C(=O)OC1CCCC1)c1cc2OCOc2cc1[N+](=O)[O-] 19047481
9927975 3943 0 ACM1 M1 receptor 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 3943 0 ACM1 M1 receptor 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
CHEMBL1223754 15696 0 ACM1 M1 receptor 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
CHEMBL1223804 15719 0 ACM1 M1 receptor 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 201692 0 ACM1 M1 receptor 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 201692 0 ACM1 M1 receptor 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
CHEMBL1223803 15718 0 ACM1 M1 receptor 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 115718 0 ACM1 M1 receptor 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 115718 0 ACM1 M1 receptor 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 184340 0 ACM1 M1 receptor 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 184340 0 ACM1 M1 receptor 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 6553 0 ACM1 M1 receptor 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 6553 0 ACM1 M1 receptor 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 187737 0 ACM1 M1 receptor 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 187737 0 ACM1 M1 receptor 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 110684 0 ACM1 M1 receptor 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 110684 0 ACM1 M1 receptor 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 6783 0 ACM1 M1 receptor 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 6783 0 ACM1 M1 receptor 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
CHEMBL1223860 15743 0 ACM1 M1 receptor 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 117312 0 ACM1 M1 receptor 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 117312 0 ACM1 M1 receptor 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 106485 0 ACM1 M1 receptor 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 106485 0 ACM1 M1 receptor 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 184184 0 ACM1 M1 receptor 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 184184 0 ACM1 M1 receptor 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 184304 0 ACM1 M1 receptor 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 184304 0 ACM1 M1 receptor 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
187 245 23 ACM1 M1 receptor 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
294 245 23 ACM1 M1 receptor 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
65 245 23 ACM1 M1 receptor 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 245 23 ACM1 M1 receptor 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 245 23 ACM1 M1 receptor 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 245 23 ACM1 M1 receptor 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
187 245 23 ACM1 M1 receptor 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
294 245 23 ACM1 M1 receptor 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
65 245 23 ACM1 M1 receptor 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 245 23 ACM1 M1 receptor 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 245 23 ACM1 M1 receptor 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 245 23 ACM1 M1 receptor 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 99832 0 ACM1 M1 receptor 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 99832 0 ACM1 M1 receptor 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 99832 0 ACM1 M1 receptor 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 115719 0 ACM1 M1 receptor 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 115719 0 ACM1 M1 receptor 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
CHEMBL1223861 15744 0 ACM1 M1 receptor 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 2796 20 ACM1 M1 receptor 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 2796 20 ACM1 M1 receptor 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 2796 20 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 187656 0 ACM1 M1 receptor 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 187656 0 ACM1 M1 receptor 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 193442 0 ACM1 M1 receptor 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 193442 0 ACM1 M1 receptor 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 17736 0 ACM1 M1 receptor 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 17736 0 ACM1 M1 receptor 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 115256 0 ACM1 M1 receptor 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 115256 0 ACM1 M1 receptor 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 6159 0 ACM1 M1 receptor 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 6159 0 ACM1 M1 receptor 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 6336 0 ACM1 M1 receptor 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 6336 0 ACM1 M1 receptor 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
CHEMBL1223941 15767 0 ACM1 M1 receptor 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 16336 0 ACM1 M1 receptor 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 16336 0 ACM1 M1 receptor 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
3652 3848 63 ACM1 M1 receptor Human 8.0 pEC50 = 8 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M1 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M1 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
57 3848 63 ACM1 M1 receptor Human 8.0 pEC50 = 8 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M1 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M1 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
60809 3848 63 ACM1 M1 receptor Human 8.0 pEC50 = 8 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M1 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M1 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
CHEMBL21536 3848 63 ACM1 M1 receptor Human 8.0 pEC50 = 8 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M1 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M1 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
DB15357 3848 63 ACM1 M1 receptor Human 8.0 pEC50 = 8 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M1 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M1 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
264734 9835 61 ACM1 M1 receptor 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 9835 61 ACM1 M1 receptor 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 115720 0 ACM1 M1 receptor 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 115720 0 ACM1 M1 receptor 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 195608 0 ACM1 M1 receptor 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 195608 0 ACM1 M1 receptor 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
118719927 115038 0 ACM1 M1 receptor Human 7.0 pEC50 = 7 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
CHEMBL3354074 115038 0 ACM1 M1 receptor Human 7.0 pEC50 = 7 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/jm501173q
46891597 6140 0 ACM1 M1 receptor 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 6140 0 ACM1 M1 receptor 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 6358 0 ACM1 M1 receptor 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 6358 0 ACM1 M1 receptor 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 16354 0 ACM1 M1 receptor 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 16354 0 ACM1 M1 receptor 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 164554 0 ACM1 M1 receptor 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 164554 0 ACM1 M1 receptor 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 135781 0 ACM1 M1 receptor 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 135781 0 ACM1 M1 receptor 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
CHEMBL2022948 73593 0 ACM1 M1 receptor 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
CHEMBL3084452 102556 0 ACM1 M1 receptor 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 6471 0 ACM1 M1 receptor 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 6471 0 ACM1 M1 receptor 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 6709 0 ACM1 M1 receptor 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 6709 0 ACM1 M1 receptor 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 6784 0 ACM1 M1 receptor 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 6784 0 ACM1 M1 receptor 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 115706 4 ACM1 M1 receptor 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 115706 4 ACM1 M1 receptor 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
187 245 23 ACM1 M1 receptor 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
294 245 23 ACM1 M1 receptor 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
65 245 23 ACM1 M1 receptor 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 245 23 ACM1 M1 receptor 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 245 23 ACM1 M1 receptor 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 245 23 ACM1 M1 receptor 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 106197 11 ACM1 M1 receptor 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 106197 11 ACM1 M1 receptor 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 136210 0 ACM1 M1 receptor 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 136210 0 ACM1 M1 receptor 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 115706 4 ACM1 M1 receptor 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 115706 4 ACM1 M1 receptor 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 117712 0 ACM1 M1 receptor 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 117712 0 ACM1 M1 receptor 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
CHEMBL4761922 180388 0 ACM1 M1 receptor 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
10236758 115029 3 ACM1 M1 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 115029 3 ACM1 M1 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
124415421 163829 1 ACM1 M1 receptor 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 163829 1 ACM1 M1 receptor 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 187895 0 ACM1 M1 receptor 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 187895 0 ACM1 M1 receptor 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 6962 0 ACM1 M1 receptor 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 6962 0 ACM1 M1 receptor 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 162717 0 ACM1 M1 receptor 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 162717 0 ACM1 M1 receptor 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 122830 0 ACM1 M1 receptor 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 122830 0 ACM1 M1 receptor 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 136210 0 ACM1 M1 receptor 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 136210 0 ACM1 M1 receptor 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 194820 0 ACM1 M1 receptor 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 194820 0 ACM1 M1 receptor 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 160511 0 ACM1 M1 receptor 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 160511 0 ACM1 M1 receptor 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
2551 750 19 ACM1 M1 receptor Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
298 750 19 ACM1 M1 receptor Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
488 750 19 ACM1 M1 receptor Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
CHEMBL965 750 19 ACM1 M1 receptor Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
DB00411 750 19 ACM1 M1 receptor Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.8b00265
CHEMBL4746155 179057 0 ACM1 M1 receptor 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 164396 0 ACM1 M1 receptor 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 164396 0 ACM1 M1 receptor 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 122200 0 ACM1 M1 receptor 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 122200 0 ACM1 M1 receptor 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 75762 0 ACM1 M1 receptor 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 75762 0 ACM1 M1 receptor 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 75779 0 ACM1 M1 receptor 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 75779 0 ACM1 M1 receptor 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
CHEMBL2024407 73756 0 ACM1 M1 receptor 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 16369 0 ACM1 M1 receptor 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 16369 0 ACM1 M1 receptor 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 67681 1 ACM1 M1 receptor 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 67681 1 ACM1 M1 receptor 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 59021 0 ACM1 M1 receptor 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 59021 0 ACM1 M1 receptor 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 67683 0 ACM1 M1 receptor 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 67683 0 ACM1 M1 receptor 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 99833 0 ACM1 M1 receptor 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 99833 0 ACM1 M1 receptor 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 195531 0 ACM1 M1 receptor 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 195531 0 ACM1 M1 receptor 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 99833 0 ACM1 M1 receptor 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 99833 0 ACM1 M1 receptor 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
CHEMBL2024418 73760 0 ACM1 M1 receptor 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 16355 0 ACM1 M1 receptor 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 16355 0 ACM1 M1 receptor 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 186743 0 ACM1 M1 receptor 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 186743 0 ACM1 M1 receptor 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 6962 0 ACM1 M1 receptor 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 6962 0 ACM1 M1 receptor 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 187572 0 ACM1 M1 receptor 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 187572 0 ACM1 M1 receptor 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 136246 0 ACM1 M1 receptor 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 136246 0 ACM1 M1 receptor 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
118719926 115037 0 ACM1 M1 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
CHEMBL3354073 115037 0 ACM1 M1 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
118724608 115717 0 ACM1 M1 receptor 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 115717 0 ACM1 M1 receptor 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
CHEMBL4755820 179861 0 ACM1 M1 receptor 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 115717 0 ACM1 M1 receptor 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 115717 0 ACM1 M1 receptor 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 160560 0 ACM1 M1 receptor 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 160560 0 ACM1 M1 receptor 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
CHEMBL3618437 122829 0 ACM1 M1 receptor 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 75763 0 ACM1 M1 receptor 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 75763 0 ACM1 M1 receptor 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
CHEMBL2336059 86919 0 ACM1 M1 receptor 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 164360 0 ACM1 M1 receptor 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 164360 0 ACM1 M1 receptor 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 6473 0 ACM1 M1 receptor 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 6473 0 ACM1 M1 receptor 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
CHEMBL1223864 15747 0 ACM1 M1 receptor 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 79811 1 ACM1 M1 receptor 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 79811 1 ACM1 M1 receptor 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 16352 0 ACM1 M1 receptor 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 16352 0 ACM1 M1 receptor 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 181106 0 ACM1 M1 receptor 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 181106 0 ACM1 M1 receptor 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 115891 0 ACM1 M1 receptor 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 115891 0 ACM1 M1 receptor 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 164674 0 ACM1 M1 receptor 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 164674 0 ACM1 M1 receptor 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
10236758 115029 3 ACM1 M1 receptor Human 6.9 pEC50 = 6.9 Binding
Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on xanomeline-induced response by BRET based Gq protein engagement assayPositive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on xanomeline-induced response by BRET based Gq protein engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 115029 3 ACM1 M1 receptor Human 6.9 pEC50 = 6.9 Binding
Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on xanomeline-induced response by BRET based Gq protein engagement assayPositive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on xanomeline-induced response by BRET based Gq protein engagement assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
62705331 75769 0 ACM1 M1 receptor 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 75769 0 ACM1 M1 receptor 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 73727 0 ACM1 M1 receptor 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 73727 0 ACM1 M1 receptor 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 73752 0 ACM1 M1 receptor 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 73752 0 ACM1 M1 receptor 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 73753 0 ACM1 M1 receptor 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 73753 0 ACM1 M1 receptor 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
CHEMBL2024408 73757 0 ACM1 M1 receptor 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 160511 0 ACM1 M1 receptor 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 160511 0 ACM1 M1 receptor 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 160560 0 ACM1 M1 receptor 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 160560 0 ACM1 M1 receptor 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 6801 0 ACM1 M1 receptor 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 6801 0 ACM1 M1 receptor 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 194072 0 ACM1 M1 receptor 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 194072 0 ACM1 M1 receptor 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
9815409 12076 11 ACM1 M1 receptor Mouse 4.9 pEC50 = 4.9 Binding
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1185481 12076 11 ACM1 M1 receptor Mouse 4.9 pEC50 = 4.9 Binding
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL416736 12076 11 ACM1 M1 receptor Mouse 4.9 pEC50 = 4.9 Binding
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
14235519 16193 8 ACM1 M1 receptor Mouse 4.9 pEC50 = 4.9 Binding
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
ChEMBL 179 1 0 4 1.1 Cc1noc(C2=CCCN(C)C2)n1 10.1021/jm960467d
CHEMBL12378 16193 8 ACM1 M1 receptor Mouse 4.9 pEC50 = 4.9 Binding
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
ChEMBL 179 1 0 4 1.1 Cc1noc(C2=CCCN(C)C2)n1 10.1021/jm960467d
145983485 164656 0 ACM1 M1 receptor 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 164656 0 ACM1 M1 receptor 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 164656 0 ACM1 M1 receptor 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 164656 0 ACM1 M1 receptor 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 164674 0 ACM1 M1 receptor 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 164674 0 ACM1 M1 receptor 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 6801 0 ACM1 M1 receptor 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 6801 0 ACM1 M1 receptor 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 160564 0 ACM1 M1 receptor 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 160564 0 ACM1 M1 receptor 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 85691 0 ACM1 M1 receptor 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 85691 0 ACM1 M1 receptor 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 195574 57 ACM1 M1 receptor 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 195574 57 ACM1 M1 receptor 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 16340 0 ACM1 M1 receptor 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 16340 0 ACM1 M1 receptor 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
3652 3848 63 ACM1 M1 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 3848 63 ACM1 M1 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 3848 63 ACM1 M1 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 3848 63 ACM1 M1 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 3848 63 ACM1 M1 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
145984808 164958 0 ACM1 M1 receptor 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 164958 0 ACM1 M1 receptor 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 122200 0 ACM1 M1 receptor 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 122200 0 ACM1 M1 receptor 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 16342 0 ACM1 M1 receptor 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 16342 0 ACM1 M1 receptor 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 67683 0 ACM1 M1 receptor 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 67683 0 ACM1 M1 receptor 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 67681 1 ACM1 M1 receptor 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 67681 1 ACM1 M1 receptor 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 67689 0 ACM1 M1 receptor 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 67689 0 ACM1 M1 receptor 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 67681 1 ACM1 M1 receptor 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 67681 1 ACM1 M1 receptor 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 160564 0 ACM1 M1 receptor 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 160564 0 ACM1 M1 receptor 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 85691 0 ACM1 M1 receptor 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 85691 0 ACM1 M1 receptor 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 750 19 ACM1 M1 receptor 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
298 750 19 ACM1 M1 receptor 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
488 750 19 ACM1 M1 receptor 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 750 19 ACM1 M1 receptor 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 750 19 ACM1 M1 receptor 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 30370 0 ACM1 M1 receptor 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 30370 0 ACM1 M1 receptor 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 119773 1 ACM1 M1 receptor 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 119773 1 ACM1 M1 receptor 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 119773 1 ACM1 M1 receptor 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
CHEMBL4764644 180605 0 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 16961 1 ACM1 M1 receptor 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 16961 1 ACM1 M1 receptor 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 2409 6 ACM1 M1 receptor 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 2409 6 ACM1 M1 receptor 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 2409 6 ACM1 M1 receptor 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
CHEMBL3633184 123317 0 ACM1 M1 receptor 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 164958 0 ACM1 M1 receptor 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 164958 0 ACM1 M1 receptor 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 199515 54 ACM1 M1 receptor 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 0 2 4 3.4 Clc1ccc2c(c1)N=C(N1CCNCC1)c1ccccc1N2 10.1021/jm100697g
CHEMBL845 199515 54 ACM1 M1 receptor 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 0 2 4 3.4 Clc1ccc2c(c1)N=C(N1CCNCC1)c1ccccc1N2 10.1021/jm100697g
57398164 67684 0 ACM1 M1 receptor 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 67684 0 ACM1 M1 receptor 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
10261985 197522 0 ACM1 M1 receptor Human 6.9 pEC50 = 6.9 Binding
In Vitro evaluation activity at the cloned Human Muscarinic acetylcholine receptor M1 determined by receptor selection and amplification technology (R-SAT)In Vitro evaluation activity at the cloned Human Muscarinic acetylcholine receptor M1 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL69306 197522 0 ACM1 M1 receptor Human 6.9 pEC50 = 6.9 Binding
In Vitro evaluation activity at the cloned Human Muscarinic acetylcholine receptor M1 determined by receptor selection and amplification technology (R-SAT)In Vitro evaluation activity at the cloned Human Muscarinic acetylcholine receptor M1 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
145961400 160826 0 ACM1 M1 receptor 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 160826 0 ACM1 M1 receptor 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 183919 0 ACM1 M1 receptor 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 183919 0 ACM1 M1 receptor 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 160745 0 ACM1 M1 receptor 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 160745 0 ACM1 M1 receptor 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
10727260 11702 0 ACM1 M1 receptor Mouse 4.9 pEC50 = 4.9 Binding
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1183133 11702 0 ACM1 M1 receptor Mouse 4.9 pEC50 = 4.9 Binding
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL281411 11702 0 ACM1 M1 receptor Mouse 4.9 pEC50 = 4.9 Binding
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
145961400 160826 0 ACM1 M1 receptor 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 160826 0 ACM1 M1 receptor 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 115710 0 ACM1 M1 receptor 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 115710 0 ACM1 M1 receptor 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 115710 0 ACM1 M1 receptor 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 115710 0 ACM1 M1 receptor 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 2409 6 ACM1 M1 receptor 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 2409 6 ACM1 M1 receptor 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 2409 6 ACM1 M1 receptor 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
647412 26922 9 ACM1 M1 receptor Rat 4.8 pEC50 = 4.8 Binding
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS binding at M1. (Class of assay: confirmatory) [Related pubchem assays: 626 ]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS binding at M1. (Class of assay: confirmatory) [Related pubchem assays: 626 ]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
CHEMBL1367424 26922 9 ACM1 M1 receptor Rat 4.8 pEC50 = 4.8 Binding
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS binding at M1. (Class of assay: confirmatory) [Related pubchem assays: 626 ]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS binding at M1. (Class of assay: confirmatory) [Related pubchem assays: 626 ]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
118663129 181887 0 ACM1 M1 receptor 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 181887 0 ACM1 M1 receptor 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 181721 0 ACM1 M1 receptor 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 181721 0 ACM1 M1 receptor 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 162980 0 ACM1 M1 receptor 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 162980 0 ACM1 M1 receptor 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 163922 0 ACM1 M1 receptor 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 163922 0 ACM1 M1 receptor 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
CHEMBL4759834 180202 0 ACM1 M1 receptor 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 16338 0 ACM1 M1 receptor 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 16338 0 ACM1 M1 receptor 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 120101 0 ACM1 M1 receptor 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 120101 0 ACM1 M1 receptor 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 120101 0 ACM1 M1 receptor 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 122202 0 ACM1 M1 receptor 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 122202 0 ACM1 M1 receptor 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 2672 2 ACM1 M1 receptor 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 2672 2 ACM1 M1 receptor 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 2672 2 ACM1 M1 receptor 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
3652 3848 63 ACM1 M1 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 3848 63 ACM1 M1 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 3848 63 ACM1 M1 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 3848 63 ACM1 M1 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 3848 63 ACM1 M1 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
46891595 6229 0 ACM1 M1 receptor 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 6229 0 ACM1 M1 receptor 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
289 233 6 ACM1 M1 receptor 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 233 6 ACM1 M1 receptor 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 233 6 ACM1 M1 receptor 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 16343 0 ACM1 M1 receptor 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 16343 0 ACM1 M1 receptor 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
CHEMBL2024426 73767 0 ACM1 M1 receptor 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 187223 0 ACM1 M1 receptor 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 187223 0 ACM1 M1 receptor 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 34730 0 ACM1 M1 receptor 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 34730 0 ACM1 M1 receptor 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
CHEMBL3618447 122838 0 ACM1 M1 receptor 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 115714 0 ACM1 M1 receptor 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 115714 0 ACM1 M1 receptor 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 115714 0 ACM1 M1 receptor 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 115714 0 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 6304 0 ACM1 M1 receptor 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 6304 0 ACM1 M1 receptor 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 6377 0 ACM1 M1 receptor 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 6377 0 ACM1 M1 receptor 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 6409 0 ACM1 M1 receptor 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 6409 0 ACM1 M1 receptor 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 6470 0 ACM1 M1 receptor 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 6470 0 ACM1 M1 receptor 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 6555 0 ACM1 M1 receptor 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 6555 0 ACM1 M1 receptor 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 6761 0 ACM1 M1 receptor 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 6761 0 ACM1 M1 receptor 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 165052 0 ACM1 M1 receptor 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 165052 0 ACM1 M1 receptor 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
90644381 111402 0 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Activation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assayActivation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assay
ChEMBL 414 5 2 4 3.1 O=C(CBr)Nc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1 10.1021/jm500556a
CHEMBL3290086 111402 0 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Activation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assayActivation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assay
ChEMBL 414 5 2 4 3.1 O=C(CBr)Nc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1 10.1021/jm500556a
2551 750 19 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
298 750 19 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
488 750 19 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
CHEMBL965 750 19 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
DB00411 750 19 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
46891029 6335 0 ACM1 M1 receptor 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 6335 0 ACM1 M1 receptor 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 6400 0 ACM1 M1 receptor 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 6400 0 ACM1 M1 receptor 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
71570775 86808 0 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
ChEMBL 444 4 0 4 4.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2013.01.017
CHEMBL2333871 86808 0 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
ChEMBL 444 4 0 4 4.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2013.01.017
145986042 165052 0 ACM1 M1 receptor 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 165052 0 ACM1 M1 receptor 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 750 19 ACM1 M1 receptor 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
298 750 19 ACM1 M1 receptor 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
488 750 19 ACM1 M1 receptor 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 750 19 ACM1 M1 receptor 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 750 19 ACM1 M1 receptor 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 750 19 ACM1 M1 receptor 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
298 750 19 ACM1 M1 receptor 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
488 750 19 ACM1 M1 receptor 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 750 19 ACM1 M1 receptor 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 750 19 ACM1 M1 receptor 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 10262 0 ACM1 M1 receptor 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 10262 0 ACM1 M1 receptor 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 164136 0 ACM1 M1 receptor 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 164136 0 ACM1 M1 receptor 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 75761 0 ACM1 M1 receptor 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 75761 0 ACM1 M1 receptor 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 16371 0 ACM1 M1 receptor 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 16371 0 ACM1 M1 receptor 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 55445 1 ACM1 M1 receptor 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 55445 1 ACM1 M1 receptor 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 55445 1 ACM1 M1 receptor 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 184385 0 ACM1 M1 receptor 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 184385 0 ACM1 M1 receptor 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
71570775 86808 0 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
ChEMBL 444 4 0 4 4.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2013.01.017
CHEMBL2333871 86808 0 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
ChEMBL 444 4 0 4 4.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2013.01.017
118124140 160590 0 ACM1 M1 receptor 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 160590 0 ACM1 M1 receptor 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 17736 0 ACM1 M1 receptor 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 17736 0 ACM1 M1 receptor 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 164335 0 ACM1 M1 receptor 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 164335 0 ACM1 M1 receptor 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 122199 0 ACM1 M1 receptor 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 122199 0 ACM1 M1 receptor 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 160596 0 ACM1 M1 receptor 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 160596 0 ACM1 M1 receptor 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
3652 3848 63 ACM1 M1 receptor Human 4.8 pEC50 = 4.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 3848 63 ACM1 M1 receptor Human 4.8 pEC50 = 4.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 3848 63 ACM1 M1 receptor Human 4.8 pEC50 = 4.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 3848 63 ACM1 M1 receptor Human 4.8 pEC50 = 4.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 3848 63 ACM1 M1 receptor Human 4.8 pEC50 = 4.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
127039038 136251 0 ACM1 M1 receptor 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 136251 0 ACM1 M1 receptor 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 19076 0 ACM1 M1 receptor 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 19076 0 ACM1 M1 receptor 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 163395 0 ACM1 M1 receptor 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 163395 0 ACM1 M1 receptor 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
118719922 115032 0 ACM1 M1 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 115032 0 ACM1 M1 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3616498 122558 0 ACM1 M1 receptor 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
CHEMBL4745827 179025 0 ACM1 M1 receptor 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
145969659 164136 0 ACM1 M1 receptor 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 164136 0 ACM1 M1 receptor 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
CHEMBL4758929 180127 0 ACM1 M1 receptor 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
1476756 195574 57 ACM1 M1 receptor Human 6.8 pEC50 = 6.8 Binding
Activation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assayActivation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assay
ChEMBL 309 4 1 4 2.8 COc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1 10.1021/jm500556a
CHEMBL608112 195574 57 ACM1 M1 receptor Human 6.8 pEC50 = 6.8 Binding
Activation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assayActivation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assay
ChEMBL 309 4 1 4 2.8 COc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1 10.1021/jm500556a
127049133 140233 0 ACM1 M1 receptor 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 140233 0 ACM1 M1 receptor 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 73729 0 ACM1 M1 receptor 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 73729 0 ACM1 M1 receptor 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 2932 37 ACM1 M1 receptor 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 2932 37 ACM1 M1 receptor 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 2932 37 ACM1 M1 receptor 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 2932 37 ACM1 M1 receptor 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 2932 37 ACM1 M1 receptor 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
1476756 195574 57 ACM1 M1 receptor Human 6.8 pEC50 = 6.8 Binding
Activation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assayActivation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assay
ChEMBL 309 4 1 4 2.8 COc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1 10.1021/jm500556a
CHEMBL608112 195574 57 ACM1 M1 receptor Human 6.8 pEC50 = 6.8 Binding
Activation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assayActivation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assay
ChEMBL 309 4 1 4 2.8 COc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1 10.1021/jm500556a
CHEMBL3084448 102552 0 ACM1 M1 receptor 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
CHEMBL3084456 102559 0 ACM1 M1 receptor 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
10465280 102073 1 ACM1 M1 receptor Human 6.8 pEC50 = 6.8 Binding
In Vitro evaluation activity at the cloned Human Muscarinic acetylcholine receptor M1 determined by receptor selection and amplification technology (R-SAT)In Vitro evaluation activity at the cloned Human Muscarinic acetylcholine receptor M1 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 196 2 1 4 1.5 CC(C)Oc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL305264 102073 1 ACM1 M1 receptor Human 6.8 pEC50 = 6.8 Binding
In Vitro evaluation activity at the cloned Human Muscarinic acetylcholine receptor M1 determined by receptor selection and amplification technology (R-SAT)In Vitro evaluation activity at the cloned Human Muscarinic acetylcholine receptor M1 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 196 2 1 4 1.5 CC(C)Oc1noc2c1CNCCC2 10.1021/jm00012a019
62705330 75768 0 ACM1 M1 receptor 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 75768 0 ACM1 M1 receptor 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 140188 0 ACM1 M1 receptor 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 140188 0 ACM1 M1 receptor 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 140233 0 ACM1 M1 receptor 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 140233 0 ACM1 M1 receptor 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 160596 0 ACM1 M1 receptor 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 160596 0 ACM1 M1 receptor 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 163487 0 ACM1 M1 receptor 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 163487 0 ACM1 M1 receptor 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
118719922 115032 0 ACM1 M1 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 115032 0 ACM1 M1 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
118729455 117102 0 ACM1 M1 receptor 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 117102 0 ACM1 M1 receptor 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 164973 0 ACM1 M1 receptor 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 164973 0 ACM1 M1 receptor 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 164973 0 ACM1 M1 receptor 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 164973 0 ACM1 M1 receptor 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 136301 0 ACM1 M1 receptor 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 136301 0 ACM1 M1 receptor 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 164402 0 ACM1 M1 receptor 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 164402 0 ACM1 M1 receptor 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 120100 0 ACM1 M1 receptor 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 120100 0 ACM1 M1 receptor 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 120100 0 ACM1 M1 receptor 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 160673 0 ACM1 M1 receptor 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 160673 0 ACM1 M1 receptor 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
139414008 163537 0 ACM1 M1 receptor Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of M1 receptor Y179A/W400A mutant (unknown origin)Positive allosteric modulation of M1 receptor Y179A/W400A mutant (unknown origin)
ChEMBL 346 2 1 2 5.1 CC(C)[C@@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4212760 163537 0 ACM1 M1 receptor Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of M1 receptor Y179A/W400A mutant (unknown origin)Positive allosteric modulation of M1 receptor Y179A/W400A mutant (unknown origin)
ChEMBL 346 2 1 2 5.1 CC(C)[C@@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL3084447 102551 0 ACM1 M1 receptor 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 199515 54 ACM1 M1 receptor 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 0 2 4 3.4 Clc1ccc2c(c1)N=C(N1CCNCC1)c1ccccc1N2 10.1021/jm100697g
CHEMBL845 199515 54 ACM1 M1 receptor 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 0 2 4 3.4 Clc1ccc2c(c1)N=C(N1CCNCC1)c1ccccc1N2 10.1021/jm100697g
137632077 155605 0 ACM1 M1 receptor Human 7.8 pEC50 = 7.8 ADMET
Positive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition by Fluo-8-AM dye based FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition by Fluo-8-AM dye based FLIPR assay
ChEMBL 417 4 1 5 2.9 Cc1cc2c(cc1Cc1ccc(-n3cccn3)cc1)C(=O)N([C@H]1CCOC[C@@H]1O)CC2 10.1021/acs.jmedchem.7b00597
CHEMBL4066701 155605 0 ACM1 M1 receptor Human 7.8 pEC50 = 7.8 ADMET
Positive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition by Fluo-8-AM dye based FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition by Fluo-8-AM dye based FLIPR assay
ChEMBL 417 4 1 5 2.9 Cc1cc2c(cc1Cc1ccc(-n3cccn3)cc1)C(=O)N([C@H]1CCOC[C@@H]1O)CC2 10.1021/acs.jmedchem.7b00597
122186861 122202 0 ACM1 M1 receptor 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 122202 0 ACM1 M1 receptor 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 122203 0 ACM1 M1 receptor 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 122203 0 ACM1 M1 receptor 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 16362 0 ACM1 M1 receptor 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 16362 0 ACM1 M1 receptor 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 31839 0 ACM1 M1 receptor 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 31839 0 ACM1 M1 receptor 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 164904 0 ACM1 M1 receptor 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 164904 0 ACM1 M1 receptor 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 41307 58 ACM1 M1 receptor 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 41307 58 ACM1 M1 receptor 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 164904 0 ACM1 M1 receptor 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 164904 0 ACM1 M1 receptor 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 186854 0 ACM1 M1 receptor 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 186854 0 ACM1 M1 receptor 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
117937668 173291 0 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of M1 AchR (unknown origin)Positive allosteric modulation of M1 AchR (unknown origin)
ChEMBL 379 5 2 5 3.1 COc1ccc(Cn2cc(C(=O)N[C@H]3CCCC[C@@H]3O)c3ncccc32)cc1 10.1021/acs.jmedchem.8b00875
CHEMBL4546244 173291 0 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of M1 AchR (unknown origin)Positive allosteric modulation of M1 AchR (unknown origin)
ChEMBL 379 5 2 5 3.1 COc1ccc(Cn2cc(C(=O)N[C@H]3CCCC[C@@H]3O)c3ncccc32)cc1 10.1021/acs.jmedchem.8b00875
71718834 86726 0 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
ChEMBL 426 4 0 4 4.5 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)cc2)cn1 10.1016/j.bmcl.2013.01.017
CHEMBL2333481 86726 0 ACM1 M1 receptor Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
ChEMBL 426 4 0 4 4.5 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)cc2)cn1 10.1016/j.bmcl.2013.01.017
146487745 179961 0 ACM1 M1 receptor 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 179961 0 ACM1 M1 receptor 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 164904 0 ACM1 M1 receptor 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 164904 0 ACM1 M1 receptor 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 164904 0 ACM1 M1 receptor 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 164904 0 ACM1 M1 receptor 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 195010 0 ACM1 M1 receptor 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 195010 0 ACM1 M1 receptor 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
71718834 86726 0 ACM1 M1 receptor Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
ChEMBL 426 4 0 4 4.5 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)cc2)cn1 10.1016/j.bmcl.2013.01.017
CHEMBL2333481 86726 0 ACM1 M1 receptor Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
ChEMBL 426 4 0 4 4.5 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)cc2)cn1 10.1016/j.bmcl.2013.01.017
146487799 181368 0 ACM1 M1 receptor 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 181368 0 ACM1 M1 receptor 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 122837 0 ACM1 M1 receptor 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 122837 0 ACM1 M1 receptor 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 164182 0 ACM1 M1 receptor 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 164182 0 ACM1 M1 receptor 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 163454 0 ACM1 M1 receptor 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 163454 0 ACM1 M1 receptor 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 136276 0 ACM1 M1 receptor 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 136276 0 ACM1 M1 receptor 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 61238 0 ACM1 M1 receptor 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 61238 0 ACM1 M1 receptor 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
137640201 156147 2 ACM1 M1 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156147 2 ACM1 M1 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
145963718 160813 0 ACM1 M1 receptor 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 160813 0 ACM1 M1 receptor 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
2551 750 19 ACM1 M1 receptor Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
298 750 19 ACM1 M1 receptor Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
488 750 19 ACM1 M1 receptor Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
CHEMBL965 750 19 ACM1 M1 receptor Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
DB00411 750 19 ACM1 M1 receptor Human 4.7 pEC50 = 4.7 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
139414015 162748 0 ACM1 M1 receptor 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 162748 0 ACM1 M1 receptor 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 16376 0 ACM1 M1 receptor 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 16376 0 ACM1 M1 receptor 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 6554 0 ACM1 M1 receptor 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 6554 0 ACM1 M1 receptor 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 6810 0 ACM1 M1 receptor 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 6810 0 ACM1 M1 receptor 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 160813 0 ACM1 M1 receptor 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 160813 0 ACM1 M1 receptor 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
10236758 115029 3 ACM1 M1 receptor Human 6.7 pEC50 = 6.7 Binding
Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on carbachol-induced response by BRET based Gq protein activation assayPositive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL3354065 115029 3 ACM1 M1 receptor Human 6.7 pEC50 = 6.7 Binding
Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on carbachol-induced response by BRET based Gq protein activation assayPositive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on carbachol-induced response by BRET based Gq protein activation assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/jm501173q
CHEMBL2024423 73764 0 ACM1 M1 receptor 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 119948 0 ACM1 M1 receptor 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 119948 0 ACM1 M1 receptor 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 140163 6 ACM1 M1 receptor 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 140163 6 ACM1 M1 receptor 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 160824 0 ACM1 M1 receptor 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 160824 0 ACM1 M1 receptor 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 160824 0 ACM1 M1 receptor 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 160824 0 ACM1 M1 receptor 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
118724607 115716 0 ACM1 M1 receptor 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 115716 0 ACM1 M1 receptor 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 115716 0 ACM1 M1 receptor 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 115716 0 ACM1 M1 receptor 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 122832 0 ACM1 M1 receptor 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 122832 0 ACM1 M1 receptor 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
CHEMBL1223938 15764 0 ACM1 M1 receptor 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 81510 2 ACM1 M1 receptor 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 81510 2 ACM1 M1 receptor 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 81510 2 ACM1 M1 receptor 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
71568899 86723 0 ACM1 M1 receptor Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
ChEMBL 444 4 0 4 4.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)cc2F)cn1 10.1016/j.bmcl.2013.01.017
CHEMBL2333477 86723 0 ACM1 M1 receptor Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
ChEMBL 444 4 0 4 4.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)cc2F)cn1 10.1016/j.bmcl.2013.01.017
71599959 86811 4 ACM1 M1 receptor Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
ChEMBL 379 3 0 5 3.0 Cn1cc(-c2ccc(CN3C(=O)C4(OCCO4)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2013.01.017
CHEMBL2333875 86811 4 ACM1 M1 receptor Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
ChEMBL 379 3 0 5 3.0 Cn1cc(-c2ccc(CN3C(=O)C4(OCCO4)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2013.01.017
10104167 1928 0 ACM1 M1 receptor 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 1928 0 ACM1 M1 receptor 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 1928 0 ACM1 M1 receptor 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 184386 1 ACM1 M1 receptor 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 184386 1 ACM1 M1 receptor 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 200712 9 ACM1 M1 receptor 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 200712 9 ACM1 M1 receptor 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 100226 0 ACM1 M1 receptor 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 100226 0 ACM1 M1 receptor 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
CHEMBL1223862 15745 0 ACM1 M1 receptor 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
CHEMBL1223939 15765 0 ACM1 M1 receptor 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
CHEMBL1223940 15766 0 ACM1 M1 receptor 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 75765 0 ACM1 M1 receptor 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 75765 0 ACM1 M1 receptor 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 16385 0 ACM1 M1 receptor 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 16385 0 ACM1 M1 receptor 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 16391 0 ACM1 M1 receptor 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 16391 0 ACM1 M1 receptor 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
CHEMBL4740865 178609 0 ACM1 M1 receptor 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 99908 0 ACM1 M1 receptor 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 99908 0 ACM1 M1 receptor 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
118719921 115031 0 ACM1 M1 receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354067 115031 0 ACM1 M1 receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
59654579 122831 0 ACM1 M1 receptor 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 122831 0 ACM1 M1 receptor 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
CHEMBL3084451 102555 0 ACM1 M1 receptor 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 55445 1 ACM1 M1 receptor 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 55445 1 ACM1 M1 receptor 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 55445 1 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 3848 63 ACM1 M1 receptor 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 53914 9 ACM1 M1 receptor 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 53914 9 ACM1 M1 receptor 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 53914 9 ACM1 M1 receptor 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 2419 4 ACM1 M1 receptor 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