Purchasability


Ligand source activities (1 row/activity)

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Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL100147 acm1_human Human No 9.7 EC50 = 0.2 nM Funct
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
341 3 0 5 3.5 C(#Cc1ccccc1)CSc1nsnc1[C@H]1CN2CCC[C@H]1C2
CHEMBL1223754 acm1_human Human No 9.4 EC50 = 0.4 nM Funct
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
403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1
CHEMBL1223804 acm1_human Human No 9.4 EC50 = 0.4 nM Funct
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
370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1
CHEMBL98255 acm1_human Human No 9.3 EC50 = 0.5 nM Funct
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC[C@H]1C2
CHEMBL1223803 acm1_human Human No 9.3 EC50 = 0.5 nM Funct
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
384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1
CHEMBL3360954 acm1_human Human No 9.2 EC50 = 0.6 nM Funct
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
373 3 1 5 3.4 Cn1cc(-c2ccc(Cn3cc4c(=O)[nH]nc-4c4ccccc43)c(F)c2)cn1
CHEMBL490797 acm1_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccc(F)cc43)CC2)CC1
CHEMBL1083925 acm1_human Human No 9.1 EC50 = 0.8 nM Funct
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
360 4 2 2 4.1 C[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1
CHEMBL522451 acm1_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(F)ccc43)CC2)CC1
CHEMBL327269 acm1_human Human No 9.0 EC50 = 1.0 nM Funct
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC1C2
CHEMBL1084850 acm1_human Human No 9.0 EC50 = 1 nM Funct
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
329 5 2 2 4.8 OC(CCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1
CHEMBL1223860 acm1_human Human No 9.0 EC50 = 1 nM Funct
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
390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1
CHEMBL340435 acm1_human Human No 9.0 EC50 = 1 nM Funct
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.
285 5 0 6 2.5 CCCSc1nsnc1OC1CN2CCCC1C2
CHEMBL316625 acm1_human Human No 9.0 EC50 = 1 nM Funct
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
341 3 0 5 3.5 C(#Cc1ccccc1)CSc1nsnc1[C@@H]1CN2CCC[C@H]1C2
CHEMBL489576 acm1_human Human No 9.0 EC50 = 1.0 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
476 4 1 4 4.8 O=c1[nH]c2cc(F)ccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1
CHEMBL490598 acm1_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4c(F)cccc43)CC2)CC1
CHEMBL667 acm1_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL667 acm1_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL291339 acm1_human Human No 9.0 EC50 = 1.1 nM Funct
In vitro functional agonism against M1 muscarinic receptor (PI)In vitro functional agonism against M1 muscarinic receptor (PI)
307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2
CHEMBL542622 acm1_human Human No 9.0 EC50 = 1.1 nM Funct
In vitro functional agonism against M1 muscarinic receptor (PI)In vitro functional agonism against M1 muscarinic receptor (PI)
307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2
CHEMBL3360955 acm1_human Human No 8.9 EC50 = 1.2 nM Funct
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
341 3 1 5 3.1 O=c1[nH]nc2c3ccccc3n(Cc3ccc(-n4cccn4)cc3)cc1-2
CHEMBL1223861 acm1_human Human No 8.9 EC50 = 1.3 nM Funct
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
390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1
CHEMBL7634 acm1_human Human Yes 8.8 EC50 = 1.6 nM Funct
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
206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1
CHEMBL21536 acm1_human Human Yes 8.8 EC50 = 1.6 nM Funct
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
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL521914 acm1_human Human No 8.8 EC50 = 1.7 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
476 4 1 4 4.8 O=c1[nH]c2c(F)cccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1
CHEMBL594432 acm1_human Human No 8.8 EC50 = 1.8 nM Funct
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
345 4 1 4 3.0 COc1ccc(Cn2cc(C(=O)O)c(=O)c3c(F)ccc(F)c32)cc1
CHEMBL126846 acm1_human Human No 8.7 EC50 = 1.9 nM Funct
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.
271 5 0 6 2.1 CCCSc1nsnc1OC1CN2CCC1C2
CHEMBL335542 acm1_human Human No 8.0 EC50 = 10 nM Funct
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
552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1
CHEMBL1082365 acm1_human Human No 8.0 EC50 = 10 nM Funct
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
378 4 2 2 4.2 C[C@H]1CNCC[C@]1(F)CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1
CHEMBL1083108 acm1_human Human No 8.0 EC50 = 10 nM Funct
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
346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1F
CHEMBL1223941 acm1_human Human No 8.0 EC50 = 10 nM Funct
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
413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1
CHEMBL1242925 acm1_human Human No 8.0 EC50 = 10 nM Funct
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
381 6 1 4 2.1 CCC(=O)NC1CCN(CCCN2C(=O)COc3cc(F)c(F)cc32)CC1
CHEMBL21536 acm1_human Human Yes 8.0 EC50 = 10 nM Bind
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
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL115581 acm1_human Human Yes 8.0 EC50 = 10 nM Funct
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
237 2 0 2 2.4 O=C1C(=O)N(Cc2ccccc2)c2ccccc21
CHEMBL3360956 acm1_human Human No 8.0 EC50 = 10 nM Funct
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
303 3 0 4 2.6 O=C1C(=O)N(Cc2ccc(-n3cccn3)cc2)c2ccccc21
CHEMBL60833 acm1_human Human No 8.0 EC50 = 10.5 nM Funct
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.
343 3 0 5 2.4 Clc1cccc(C#CCOc2nsnc2C23CN4CC2C3C4)c1
CHEMBL3354074 acm1_human Human No 7.0 EC50 = 100 nM Bind
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
386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1
CHEMBL1082316 acm1_human Human No 7.0 EC50 = 100 nM Funct
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
362 4 2 2 4.4 O=C(NCC1CCNCC1)c1ccc(Cl)cc1-c1cccc(Cl)c1
CHEMBL1083277 acm1_human Human No 7.0 EC50 = 100 nM Funct
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
362 4 2 2 4.4 O=C(NCC1CCNCC1)c1cc(Cl)ccc1-c1cccc(Cl)c1
CHEMBL1243138 acm1_human Human No 7.0 EC50 = 100 nM Funct
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
423 7 1 4 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CSc3ccccc32)CC1
CHEMBL4237601 acm1_rat Rat No 7.0 EC50 = 100 nM Funct
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
448 5 2 7 3.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)N[C@@H]3CCOC[C@H]3O)nc21
CHEMBL373888 acm1_human Human No 6.0 EC50 = 1000 nM Funct
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
399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1
CHEMBL2022948 acm1_human Human No 6.0 EC50 = 1000 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
351 6 2 5 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cccs1)C2
CHEMBL3084452 acm1_human Human No 6.0 EC50 = 1000 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
351 6 2 4 2.1 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)C1CCCCC1
CHEMBL1083718 acm1_human Human No 6.0 EC50 = 1000 nM Funct
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
342 4 2 2 4.0 Cc1ccc(-c2cccc(Cl)c2)c(C(=O)NCC2CCNCC2)c1
CHEMBL1084572 acm1_human Human No 6.0 EC50 = 1000 nM Funct
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
346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1F
CHEMBL1084851 acm1_human Human No 6.0 EC50 = 1000 nM Funct
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
311 4 1 1 5.4 Clc1cccc(-c2ccccc2/C=C/CC2CCNCC2)c1
CHEMBL3360928 acm1_human Human Yes 6.0 EC50 = 1000 nM Funct
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
383 4 0 4 4.5 O=c1c2cn(Cc3ccccc3)c3ccccc3c-2nn1Cc1ccccc1F
CHEMBL667 acm1_human Human Yes 4.0 EC50 = 100000 nM Funct
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
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL314737 acm1_human Human Yes 4.0 EC50 = 100000 nM Funct
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
180 1 1 5 0.1 Nc1noc(C2CN3CCC2C3)n1
CHEMBL3745973 acm1_human Human No 7.0 EC50 = 101 nM Funct
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
415 5 2 6 3.3 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12
CHEMBL3360928 acm1_human Human Yes 6.0 EC50 = 1010 nM Funct
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
383 4 0 4 4.5 O=c1c2cn(Cc3ccccc3)c3ccccc3c-2nn1Cc1ccccc1F
CHEMBL341242 acm1_human Human No 7.0 EC50 = 102 nM Funct
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.
283 6 0 6 2.2 CCCCOc1nsnc1OC1CN2CCC1CC2
CHEMBL4761922 acm1_human Human No 7.0 EC50 = 102 nM Funct
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
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
CHEMBL3354065 acm1_human Human Yes 7.0 EC50 = 102.3 nM Bind
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
328 7 0 2 4.3 CCCCC1CCN(CC1)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL4216615 acm1_human Human No 7.0 EC50 = 103 nM Funct
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
300 1 1 2 4.3 C[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S
CHEMBL523657 acm1_human Human No 6.0 EC50 = 1030 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
438 4 1 4 4.6 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1
CHEMBL1085686 acm1_rat Rat No 6.0 EC50 = 1030 nM Funct
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])]
371 3 0 4 3.2 Cn1cc(-c2cc(F)c(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1
CHEMBL4202915 acm1_human Human No 7.0 EC50 = 104 nM Funct
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
342 3 1 2 5.5 CCC[C@]1(C)N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S
CHEMBL3618439 acm1_human Human No 7.0 EC50 = 105 nM Funct
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
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
CHEMBL3745973 acm1_human Human No 7.0 EC50 = 106 nM Funct
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
415 5 2 6 3.3 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12
CHEMBL60374 acm1_human Human No 7.0 EC50 = 107 nM Funct
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.
359 3 0 5 3.1 Clc1ccc(C#CCSc2nsnc2C23CN4CC2C3C4)cc1
CHEMBL4125749 acm1_human Human No 6.0 EC50 = 1071.5 nM Funct
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
445 4 2 5 3.0 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(Br)nc2)c2ccccc2O1
CHEMBL965 acm1_human Human Yes 5.0 EC50 = 10715.2 nM Bind
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
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL4746155 acm1_human Human No 7.0 EC50 = 108 nM Funct
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
456 6 2 6 4.0 COc1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nn4cccc34)cc2)cn1
CHEMBL4229092 acm1_human Human No 7.0 EC50 = 109 nM Funct
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
392 5 2 6 2.0 Cc1cnc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1
CHEMBL3608419 acm1_human Human No 8.0 EC50 = 11.1 nM Funct
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
431 5 2 7 2.4 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2)cn1
CHEMBL2059306 acm1_human Human No 7.0 EC50 = 110 nM Funct
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
404 5 1 4 3.3 O=C1CCc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1
CHEMBL2059324 acm1_human Human No 7.0 EC50 = 110 nM Funct
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
424 5 1 5 2.9 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3c(F)cccc32)CC1
CHEMBL2024407 acm1_human Human No 7.0 EC50 = 110 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](NCCNC(=O)c1ccccc1)C2
CHEMBL1243267 acm1_human Human No 7.0 EC50 = 110 nM Funct
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
357 6 1 4 1.8 O=C(NC1CCN(CCCN2C(=O)COc3ccccc32)CC1)C1CC1
CHEMBL1916224 acm1_rat Rat No 7.0 EC50 = 110 nM Funct
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
373 4 1 4 2.8 CCOC(=O)N1CCC(CC1)N2CCC[C@H](C2)NC(=O)C3=CC=CC=C3C
CHEMBL171721 acm1_rat Rat No 7.0 EC50 = 110 nM Funct
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)
193 1 0 4 1.0 Cc1noc(C2(C)CN3CCC2C3)n1
CHEMBL1916226 acm1_rat Rat No 7.0 EC50 = 110 nM Funct
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
359 4 1 4 2.5 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3)C2)CC1
CHEMBL291351 acm1_human Human No 7.0 EC50 = 110 nM Funct
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1
CHEMBL60777 acm1_human Human No 7.0 EC50 = 110 nM Funct
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.
361 3 0 5 2.6 Fc1cc(Cl)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1
CHEMBL291351 acm1_human Human No 7.0 EC50 = 110.9 nM Funct
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.
311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1
CHEMBL2024418 acm1_human Human No 6.0 EC50 = 1100 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
359 6 2 4 2.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1C)C2
CHEMBL1243139 acm1_human Human No 6.0 EC50 = 1100 nM Funct
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
393 7 1 5 2.8 O=C(Cc1ccccc1)NC1CCN(CCCn2c(=O)oc3ccccc32)CC1
CHEMBL514689 acm1_human Human No 6.0 EC50 = 1100 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
469 5 1 6 4.2 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3[N+](=O)[O-])CC2)CC1
CHEMBL1085686 acm1_human Human No 6.0 EC50 = 1100 nM Funct
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
371 3 0 4 3.2 Cn1cc(-c2cc(F)c(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1
CHEMBL521388 acm1_human Human No 5.0 EC50 = 11100 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
506 3 1 4 4.9 O=C(c1ccccc1C(F)(F)F)N1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1
CHEMBL3746514 acm1_human Human No 7.0 EC50 = 112 nM Funct
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
402 6 1 6 2.1 CN(C)C(=O)CNC(=O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12
CHEMBL3354073 acm1_human Human No 7.0 EC50 = 112.2 nM Bind
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
358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1
CHEMBL3360950 acm1_human Human No 5.9 EC50 = 1148.2 nM Funct
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
459 5 0 6 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-n5cccn5)cc4)cc-3c2=O)c(C)c1
CHEMBL4755820 acm1_human Human No 6.9 EC50 = 115 nM Funct
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
409 5 2 5 2.8 Cc1cc(F)c(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1
CHEMBL3360950 acm1_human Human No 5.9 EC50 = 1150 nM Funct
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
459 5 0 6 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-n5cccn5)cc4)cc-3c2=O)c(C)c1
CHEMBL4126348 acm1_human Human No 5.9 EC50 = 1174.9 nM Funct
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
418 5 2 6 2.7 O=C(N[C@H]1CCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL3618437 acm1_human Human No 6.9 EC50 = 118 nM Funct
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
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
CHEMBL2059307 acm1_human Human No 7.9 EC50 = 12 nM Funct
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
405 5 1 5 2.7 O=C1CCc2ncccc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1
CHEMBL2336059 acm1_human Human No 7.9 EC50 = 12 nM Funct
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
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
CHEMBL4228557 acm1_human Human No 7.9 EC50 = 12 nM Funct
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
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
CHEMBL1083723 acm1_human Human No 7.9 EC50 = 12.6 nM Funct
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
342 4 2 2 4.0 Cc1ccc(-c2ccccc2C(=O)NCC2CCNCC2)cc1Cl
CHEMBL1223864 acm1_human Human No 7.9 EC50 = 12.6 nM Funct
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
436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1
CHEMBL2146597 acm1_human Human Yes 7.9 EC50 = 12.6 nM Funct
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
299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1
CHEMBL1243109 acm1_human Human No 6.9 EC50 = 120 nM Funct
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
435 8 1 4 3.2 COc1ccc2c(c1)N(CCCN1CCC(NC(=O)Cc3ccccc3)CC1)C(=O)CC2
CHEMBL478034 acm1_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
435 5 1 6 3.5 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3[N+](=O)[O-])CC2)CC1
CHEMBL336933 acm1_human Human No 6.9 EC50 = 120 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
550 14 0 10 6.4 CN1CCC=C(c2nsnc2SCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1
CHEMBL4240517 acm1_human Human No 6.9 EC50 = 120 nM Funct
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
444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1
CHEMBL3354065 acm1_human Human Yes 6.9 EC50 = 120.2 nM Bind
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
328 7 0 2 4.3 CCCCC1CCN(CC1)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL2059314 acm1_human Human No 5.9 EC50 = 1200 nM Funct
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
407 5 1 6 2.2 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3ccncc32)CC1
CHEMBL2024328 acm1_human Human No 5.9 EC50 = 1200 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
359 5 1 4 2.4 CCOC(=O)N1CC[C@H]2[C@H](CCCN2CCNC(=O)c2ccccc2)C1
CHEMBL2024403 acm1_human Human No 5.9 EC50 = 1200 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
371 4 1 4 2.6 CCOC(=O)N1C2CCC1CC(N1CC[C@H](NC(=O)c3ccccc3)C1)C2
CHEMBL2024404 acm1_human Human No 5.9 EC50 = 1200 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
385 4 1 4 3.0 CCOC(=O)N1C2CCC1CC(N1CC[C@@H](NC(=O)c3ccccc3C)C1)C2
CHEMBL2024408 acm1_human Human No 5.9 EC50 = 1200 nM Funct
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1)C2
CHEMBL4125749 acm1_human Human No 5.9 EC50 = 1200 nM Funct
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
445 4 2 5 3.0 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(Br)nc2)c2ccccc2O1
CHEMBL4126348 acm1_human Human No 5.9 EC50 = 1200 nM Funct
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
418 5 2 6 2.7 O=C(N[C@H]1CCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL1084940 acm1_human Human No 5.9 EC50 = 1200 nM Funct
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
371 3 0 4 3.2 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4c(F)ccc(F)c43)c(F)c2)cn1
CHEMBL59862 acm1_human Human No 5.9 EC50 = 1200 nM Funct
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.
376 3 0 4 4.6 Clc1cc(Cl)cc(C#CCOc2nsnc2C23CC4CC2C3C4)c1
CHEMBL1185481 acm1_mouse Mouse Yes 4.9 EC50 = 12000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1
CHEMBL416736 acm1_mouse Mouse Yes 4.9 EC50 = 12000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1
CHEMBL12378 acm1_mouse Mouse Yes 4.9 EC50 = 12000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
179 1 0 4 1.1 Cc1noc(C2=CCCN(C)C2)n1
CHEMBL4240041 acm1_rat Rat No 5.9 EC50 = 1202.3 nM Funct
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
444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1
CHEMBL4240041 acm1_rat Rat No 5.9 EC50 = 1210 nM Funct
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
444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1
CHEMBL4240517 acm1_human Human No 6.9 EC50 = 123.0 nM Funct
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
444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1
CHEMBL1084940 acm1_rat Rat No 5.9 EC50 = 1230 nM Funct
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])]
371 3 0 4 3.2 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4c(F)ccc(F)c43)c(F)c2)cn1
CHEMBL4126400 acm1_human Human No 5.9 EC50 = 1258.9 nM Funct
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
447 5 2 7 2.7 Cn1nccc1-c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1
CHEMBL2313530 acm1_human Human No 5.9 EC50 = 1258.9 nM Funct
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
336 3 1 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(N)c4ccccc43)c(F)c2)cn1
CHEMBL608112 acm1_human Human Yes 6.9 EC50 = 128.8 nM Funct
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
309 4 1 4 2.8 COc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1
CHEMBL1242979 acm1_human Human No 7.9 EC50 = 13 nM Funct
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
501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC
CHEMBL21536 acm1_human Human Yes 7.9 EC50 = 13.2 nM Bind
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
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL4247625 acm1_rat Rat No 7.9 EC50 = 13.8 nM Funct
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
446 5 2 8 1.8 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cn2)n1
CHEMBL3608419 acm1_rat Rat No 7.9 EC50 = 13.8 nM Funct
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
431 5 2 7 2.4 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2)cn1
CHEMBL1243010 acm1_human Human No 6.9 EC50 = 130 nM Funct
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
437 8 1 5 2.6 COc1cccc(CC(=O)NC2CCN(CCCN3C(=O)COc4ccccc43)CC2)c1
CHEMBL1916226 acm1_rat Rat No 6.9 EC50 = 130 nM Funct
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
359 4 1 4 2.5 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3)C2)CC1
CHEMBL1916224 acm1_human Human No 5.9 EC50 = 1300 nM Funct
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
373 4 1 4 2.8 CCOC(=O)N1CCC(CC1)N2CCC[C@H](C2)NC(=O)C3=CC=CC=C3C
CHEMBL1916232 acm1_rat Rat No 5.9 EC50 = 1300 nM Funct
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
365 4 1 5 2.6 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccs3)C2)CC1
CHEMBL1916224 acm1_rat Rat No 5.9 EC50 = 1300 nM Funct
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
373 4 1 4 2.8 CCOC(=O)N1CCC(CC1)N2CCC[C@H](C2)NC(=O)C3=CC=CC=C3C
CHEMBL4126400 acm1_human Human No 5.9 EC50 = 1300 nM Funct
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
447 5 2 7 2.7 Cn1nccc1-c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1
CHEMBL2313530 acm1_human Human No 5.9 EC50 = 1300 nM Funct
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
336 3 1 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(N)c4ccccc43)c(F)c2)cn1
CHEMBL965 acm1_human Human Yes 4.9 EC50 = 13000 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL139603 acm1_human Human No 4.9 EC50 = 13000 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
592 17 0 10 7.6 CN1CCC=C(c2nsnc2SCCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1
CHEMBL3310802 acm1_human Human Yes 6.9 EC50 = 133 nM Funct
Agonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assayAgonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assay
429 3 0 5 2.8 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(C(=O)N(C)C)c2ncccc23)CC1
CHEMBL3545481 acm1_human Human Yes 6.9 EC50 = 133 nM Funct
Agonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assayAgonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assay
429 3 0 5 2.8 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(C(=O)N(C)C)c2ncccc23)CC1
CHEMBL4764644 acm1_human Human No 6.9 EC50 = 133 nM Funct
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
426 5 2 5 4.0 O=C(N[C@@H]1CCCC[C@H]1O)c1cc(Cc2ccc(-c3ccncc3)cc2)c2cccn2n1
CHEMBL21536 acm1_human Human Yes 6.9 EC50 = 134.5 nM Funct
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.
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL125732 acm1_human Human Yes 6.9 EC50 = 135.8 nM Funct
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.
313 7 0 6 3.3 CCCCCSc1nsnc1OC1CN2CCC1CC2
CHEMBL1357815 acm1_rat Rat Yes 5.9 EC50 = 1380 nM Funct
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
505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F
CHEMBL3633184 acm1_human Human No 7.9 EC50 = 14 nM Funct
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
412 4 1 4 3.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@@H](N3Cc4ccccc4NC3=O)C1)C2
CHEMBL4247625 acm1_rat Rat No 7.9 EC50 = 14 nM Funct
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
446 5 2 8 1.8 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cn2)n1
CHEMBL845 acm1_human Human Yes 6.9 EC50 = 140 nM Funct
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
312 0 2 4 3.4 C1CN(CCN1)C2=NC3=C(C=CC(=C3)Cl)NC4=CC=CC=C42
CHEMBL1916227 acm1_rat Rat No 6.9 EC50 = 140 nM Funct
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
377 4 1 4 2.6 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(F)c3)C2)CC1
CHEMBL69306 acm1_human Human No 6.9 EC50 = 140 nM Bind
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)
192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2
CHEMBL4130291 acm1_human Human No 6.9 EC50 = 140 nM Funct
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
450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cccc(F)c2O1
CHEMBL487762 acm1_human Human No 5.9 EC50 = 1400 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
440 4 1 5 2.8 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1
CHEMBL4129005 acm1_human Human No 5.9 EC50 = 1400 nM Funct
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
430 5 2 5 3.5 O=C(N[C@H]1CCCC[C@@H]1O)C1Cc2ccccc2N(Cc2ccc(-n3cccn3)cc2)C1
CHEMBL1183133 acm1_mouse Mouse No 4.9 EC50 = 14000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1
CHEMBL281411 acm1_mouse Mouse No 4.9 EC50 = 14000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1
CHEMBL4130291 acm1_human Human No 6.9 EC50 = 141.3 nM Funct
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
450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cccc(F)c2O1
CHEMBL3360939 acm1_human Human No 5.9 EC50 = 1412.5 nM Funct
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
411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccc(F)c4)cc-3c2=O)c(C)c1
CHEMBL3360939 acm1_human Human No 5.9 EC50 = 1420 nM Funct
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
411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccc(F)c4)cc-3c2=O)c(C)c1
CHEMBL1357815 acm1_rat Rat Yes 5.9 EC50 = 1424 nM Funct
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])]
505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F
CHEMBL1367424 acm1_rat Rat Yes 4.8 EC50 = 14360 nM Bind
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 ]
325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1
CHEMBL4790220 acm1_human Human No 6.8 EC50 = 144 nM Funct
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
393 5 2 6 2.5 Cc1cnc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-c2cocn2)cc1
CHEMBL4788148 acm1_human Human No 6.8 EC50 = 146 nM Funct
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
451 5 2 6 3.9 N#Cc1cncc(-c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)nn4cccc34)cc2)c1
CHEMBL4206098 acm1_human Human No 5.8 EC50 = 1465 nM Funct
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
380 2 1 2 5.8 Fc1ccccc1C1=N[C@@H](c2ccccc2)C(=S)Nc2ccc(Cl)cc21
CHEMBL4217684 acm1_human Human No 5.8 EC50 = 1469 nM Funct
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
370 3 1 2 6.0 CC(C)[C@@H]1N=C(c2ccccc2)c2cc(-c3ccccc3)ccc2NC1=S
CHEMBL4759834 acm1_human Human No 6.8 EC50 = 149 nM Funct
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
444 5 2 5 4.2 O=C(N[C@@H]1CCCC[C@H]1O)c1cc(Cc2ccc(-c3ccc(F)cn3)cc2)c2cccn2n1
CHEMBL1242951 acm1_human Human No 7.8 EC50 = 15 nM Funct
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
441 7 1 3 3.5 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3cc(F)c(F)cc32)CC1
CHEMBL3414842 acm1_human Human No 7.8 EC50 = 15.5 nM Funct
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
621 12 1 6 4.9 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Br)ccc2c1=O
CHEMBL3559129 acm1_human Human No 7.8 EC50 = 15.5 nM Funct
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
621 12 1 6 4.9 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Br)ccc2c1=O
CHEMBL3608421 acm1_human Human No 7.8 EC50 = 15.5 nM Funct
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
449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2F)cn1
CHEMBL99521 acm1_human Human Yes 7.8 EC50 = 15.7 nM Funct
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1
CHEMBL21536 acm1_human Human Yes 7.8 EC50 = 15.9 nM Bind
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
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL1082680 acm1_human Human No 7.8 EC50 = 15.9 nM Funct
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
346 4 2 2 3.9 O=C(NCC1CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1
CHEMBL1242950 acm1_human Human Yes 6.8 EC50 = 150 nM Funct
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
301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C
CHEMBL1243011 acm1_human Human No 6.8 EC50 = 150 nM Funct
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
423 7 1 3 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3c(F)cccc32)CC1
CHEMBL2024426 acm1_human Human No 5.8 EC50 = 1500 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
351 6 2 4 2.4 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)C1CCCCC1)C2
CHEMBL518747 acm1_human Human No 5.8 EC50 = 1500 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
492 4 1 4 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1
CHEMBL143466 acm1_human Human No 5.8 EC50 = 1500 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
578 16 0 10 7.2 CN1CCC=C(c2nsnc2SCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1
CHEMBL3618447 acm1_human Human No 6.8 EC50 = 154 nM Funct
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
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
CHEMBL3360946 acm1_human Human No 5.8 EC50 = 1548.8 nM Funct
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
394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccncc4)cc-3c2=O)c(C)c1
CHEMBL3360946 acm1_human Human No 5.8 EC50 = 1550 nM Funct
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
394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccncc4)cc-3c2=O)c(C)c1
CHEMBL21536 acm1_human Human Yes 6.8 EC50 = 158.5 nM Funct
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
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL21536 acm1_human Human Yes 6.8 EC50 = 158.5 nM Funct
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
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL1083003 acm1_human Human No 6.8 EC50 = 158.5 nM Funct
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
364 4 2 2 3.8 O=C(NC[C@H]1CCNC[C@H]1F)c1c(F)cccc1-c1cccc(Cl)c1
CHEMBL1083317 acm1_human Human No 6.8 EC50 = 158.5 nM Funct
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
396 4 2 2 4.7 O=C(NCC1=C(F)CNCC1)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F
CHEMBL1083419 acm1_human Human No 6.8 EC50 = 158.5 nM Funct
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
342 4 2 2 4.0 Cc1ccc(Cl)cc1-c1ccccc1C(=O)NCC1CCNCC1
CHEMBL1083717 acm1_human Human No 6.8 EC50 = 158.5 nM Funct
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
342 4 2 2 4.0 Cc1ccc(C(=O)NCC2CCNCC2)c(-c2cccc(Cl)c2)c1
CHEMBL1083927 acm1_human Human No 6.8 EC50 = 158.5 nM Funct
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
392 4 2 2 4.7 CC1CNCC=C1CNC(=O)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F
CHEMBL1084804 acm1_human Human No 6.8 EC50 = 158.5 nM Funct
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
328 4 2 2 3.4 O=C(Cc1ccccc1-c1cccc(Cl)c1)NC1CCNCC1
CHEMBL4249357 acm1_rat Rat No 5.8 EC50 = 1580 nM Funct
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
444 6 1 7 3.1 Cn1ccc(-c2ccc(Cc3cc(C(=O)NCC4CCOCC4)nc4c3ccn4C)cn2)n1
CHEMBL3290086 acm1_human Human No 5.8 EC50 = 1584.9 nM Bind
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
414 5 2 4 3.1 O=C(CBr)Nc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1
CHEMBL965 acm1_human Human Yes 5.8 EC50 = 1584.9 nM Bind
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
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL1083107 acm1_human Human No 5.8 EC50 = 1584.9 nM Funct
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
342 4 2 2 4.0 Cc1cc(Cl)cc(-c2ccccc2C(=O)NCC2CCNCC2)c1
CHEMBL1083401 acm1_human Human No 5.8 EC50 = 1584.9 nM Funct
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
410 6 1 3 3.9 CS(=O)(=O)N(Cc1c(F)cccc1-c1cccc(Cl)c1)CC1CCNCC1
CHEMBL2333871 acm1_human Human No 5.8 EC50 = 1584.9 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
444 4 0 4 4.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)c(F)c2)cn1
CHEMBL4249357 acm1_rat Rat No 5.8 EC50 = 1584.9 nM Funct
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
444 6 1 7 3.1 Cn1ccc(-c2ccc(Cc3cc(C(=O)NCC4CCOCC4)nc4c3ccn4C)cn2)n1
CHEMBL965 acm1_human Human Yes 4.8 EC50 = 15848.9 nM Funct
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
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL965 acm1_human Human Yes 4.8 EC50 = 15848.9 nM Funct
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
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL1169506 acm1_human Human No 6.8 EC50 = 159 nM Funct
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CC[C@@H]1C2
CHEMBL4225188 acm1_human Human No 7.8 EC50 = 16 nM Funct
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
431 5 3 7 2.3 O=C(N[C@H]1CCC(O)C[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12
CHEMBL2059305 acm1_human Human No 6.8 EC50 = 160 nM Funct
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
387 5 1 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(c2ccc3[nH]ccc3c2)CC1
CHEMBL1243295 acm1_human Human No 6.8 EC50 = 160 nM Funct
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
371 6 1 4 2.2 O=C(NC1CCN(CCCN2C(=O)COc3ccccc32)CC1)C1CCC1
CHEMBL1624037 acm1_human Human No 5.8 EC50 = 1600 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
333 6 2 4 1.9 CCOC(=O)N1CCC(CC1)NCCNC(=O)C2=CC=CC=C2C
CHEMBL491208 acm1_human Human No 5.8 EC50 = 1600 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
449 4 1 5 4.2 N#Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1
CHEMBL2333871 acm1_human Human No 5.8 EC50 = 1600 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
444 4 0 4 4.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)c(F)c2)cn1
CHEMBL4126807 acm1_human Human No 5.8 EC50 = 1600 nM Funct
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
450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2F)c2ccccc2O1
CHEMBL126846 acm1_human Human No 6.8 EC50 = 161.7 nM Funct
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.
271 5 0 6 2.1 CCCSc1nsnc1OC1CN2CCC1C2
CHEMBL4228097 acm1_human Human No 6.8 EC50 = 162 nM Funct
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
425 5 3 7 2.3 Cc1cnc(C(=O)N[C@H]2CCOC(O)[C@@H]2O)cc1Cc1ccc(-c2cscn2)cc1
CHEMBL3608418 acm1_rat Rat No 6.8 EC50 = 162.5 nM Funct
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
405 4 2 7 1.9 Cn1ncc2cc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)ccc21
CHEMBL4126841 acm1_human Human No 5.8 EC50 = 1621.8 nM Funct
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
441 6 1 7 3.7 COc1cccnc1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL21536 acm1_human Human Yes 4.8 EC50 = 16218.1 nM Bind
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
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL3746599 acm1_human Human No 6.8 EC50 = 163 nM Funct
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
414 5 2 5 3.9 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2ccccc12
CHEMBL129764 acm1_human Human No 6.8 EC50 = 164.8 nM Funct
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.
297 7 0 6 2.6 CCCCCOc1nsnc1OC1CN2CCC1CC2
CHEMBL4211028 acm1_human Human No 6.8 EC50 = 165 nM Funct
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
344 2 1 2 4.8 Fc1ccccc1C1=N[C@@H](C2CC2)C(=S)Nc2ccc(Cl)cc21
CHEMBL3354068 acm1_human Human No 6.8 EC50 = 166.0 nM Bind
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
565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1
CHEMBL3616498 acm1_human Human No 6.8 EC50 = 166 nM Funct
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
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
CHEMBL4745827 acm1_human Human No 6.8 EC50 = 166 nM Funct
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
437 5 2 6 3.4 Cc1c(Cc2ccc(-c3cscn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C
CHEMBL4225188 acm1_human Human No 6.8 EC50 = 167 nM Funct
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
431 5 3 7 2.3 O=C(N[C@H]1CCC(O)C[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12
CHEMBL4758929 acm1_human Human No 5.8 EC50 = 1686 nM Funct
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
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
CHEMBL608112 acm1_human Human Yes 6.8 EC50 = 169.8 nM Bind
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
309 4 1 4 2.8 COc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1
CHEMBL3823999 acm1_rat Rat No 5.8 EC50 = 1698.2 nM Funct
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
393 3 0 4 3.7 Cn1cc2c(-c3cc(F)c(CN4C=CC5=NCCN5C4=O)c(F)c3)cccc2n1
CHEMBL2024331 acm1_human Human No 7.8 EC50 = 17 nM Funct
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3C)C1)C2
CHEMBL550 acm1_human Human Yes 7.8 EC50 = 17.5 nM Funct
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
208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C
CHEMBL608112 acm1_human Human Yes 6.8 EC50 = 170 nM Bind
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
309 4 1 4 2.8 COc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1
CHEMBL3084448 acm1_human Human No 6.8 EC50 = 170 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
359 6 2 4 2.2 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1C
CHEMBL3084456 acm1_human Human No 6.8 EC50 = 170 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
351 6 2 5 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccs1
CHEMBL305264 acm1_human Human Yes 6.8 EC50 = 170 nM Bind
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)
196 2 1 4 1.5 CC(C)Oc1noc2c1CNCCC2
CHEMBL2059313 acm1_human Human No 5.8 EC50 = 1700 nM Funct
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
407 5 1 6 2.2 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3cccnc32)CC1
CHEMBL3823424 acm1_rat Rat No 5.8 EC50 = 1700 nM Funct
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
393 3 0 5 3.4 Cn1cc2cc(-c3cc(F)c(CN4CCn5nccc5C4=O)c(F)c3)ccc2n1
CHEMBL3823999 acm1_rat Rat No 5.8 EC50 = 1700 nM Funct
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
393 3 0 4 3.7 Cn1cc2c(-c3cc(F)c(CN4C=CC5=NCCN5C4=O)c(F)c3)cccc2n1
CHEMBL4126841 acm1_human Human No 5.8 EC50 = 1700 nM Funct
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
441 6 1 7 3.7 COc1cccnc1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL4212268 acm1_human Human No 6.8 EC50 = 172 nM Funct
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
362 2 1 2 5.6 CC(C)[C@@H]1N=C(c2cccc(Cl)c2)c2cc(Cl)ccc2NC1=S
CHEMBL3354068 acm1_human Human No 6.8 EC50 = 173.8 nM Bind
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
565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1
CHEMBL3402922 acm1_human Human No 4.8 EC50 = 17320 nM Funct
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
182 1 1 4 0.3 CN1CCC=C(C2=NOC(O)C2)C1
CHEMBL4248069 acm1_rat Rat No 5.8 EC50 = 1737.8 nM Funct
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
432 5 1 6 4.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)NC3CCOCC3)nc21
CHEMBL4248069 acm1_rat Rat No 5.8 EC50 = 1740 nM Funct
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
432 5 1 6 4.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)NC3CCOCC3)nc21
CHEMBL3747254 acm1_human Human No 6.8 EC50 = 175 nM Funct
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
401 6 1 6 3.2 O=C(NC[C@@H]1CCCO1)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12
CHEMBL4229133 acm1_human Human No 6.8 EC50 = 177 nM Funct
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
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
CHEMBL3414841 acm1_human Human No 6.8 EC50 = 177.8 nM Funct
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
561 12 1 6 4.3 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2c(F)cccc2c1=O
CHEMBL3559128 acm1_human Human No 6.8 EC50 = 177.8 nM Funct
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
561 12 1 6 4.3 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2c(F)cccc2c1=O
CHEMBL4128022 acm1_human Human No 6.8 EC50 = 177.8 nM Funct
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
447 5 2 7 2.7 Cn1cc(-c2ccc(CN3CC(C(=O)N[C@H]4CCCC[C@@H]4O)Oc4ccccc43)cn2)cn1
CHEMBL4212760 acm1_human Human No 6.8 EC50 = 178 nM Bind
Positive allosteric modulation of M1 receptor Y179A/W400A mutant (unknown origin)Positive allosteric modulation of M1 receptor Y179A/W400A mutant (unknown origin)
346 2 1 2 5.1 CC(C)[C@@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S
CHEMBL3084447 acm1_human Human No 7.8 EC50 = 18 nM Funct
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
345 6 2 4 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1
CHEMBL845 acm1_human Human Yes 7.8 EC50 = 18 nM Funct
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
312 0 2 4 3.4 C1CN(CCN1)C2=NC3=C(C=CC(=C3)Cl)NC4=CC=CC=C42
CHEMBL4066701 acm1_human Human No 7.8 EC50 = 18 nM Funct
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
417 4 1 5 2.9 Cc1cc2c(cc1Cc1ccc(-n3cccn3)cc1)C(=O)N([C@H]1CCOC[C@@H]1O)CC2
CHEMBL3608421 acm1_rat Rat No 7.8 EC50 = 18 nM Funct
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
449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2F)cn1
CHEMBL3608422 acm1_rat Rat No 7.8 EC50 = 18 nM Funct
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
408 5 3 6 1.3 CNC(=O)c1ccc(Cn2cc(C(=O)N[C@H]3COCC[C@@H]3O)c3ncccc32)cc1
CHEMBL1243202 acm1_human Human No 6.8 EC50 = 180 nM Funct
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
331 5 1 4 1.4 CC(=O)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1
CHEMBL140985 acm1_human Human No 6.8 EC50 = 180 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
522 12 0 10 5.7 CN1CCC=C(c2nsnc2SCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1
CHEMBL4246159 acm1_human Human No 6.8 EC50 = 180 nM Funct
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
443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1
CHEMBL1492697 acm1_human Human Yes 6.8 EC50 = 180 nM Funct
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
286 1 1 2 4.2 SC1=Nc2ccc(Cl)cc2C(c2ccccc2)=NC1
CHEMBL4246159 acm1_rat Rat No 6.8 EC50 = 180 nM Funct
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
443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1
CHEMBL515489 acm1_human Human No 5.8 EC50 = 1800 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
458 4 1 4 4.9 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3Cl)CC2)CC1
CHEMBL4546244 acm1_human Human No 5.8 EC50 = 1800 nM Bind
Positive allosteric modulation of M1 AchR (unknown origin)Positive allosteric modulation of M1 AchR (unknown origin)
379 5 2 5 3.1 COc1ccc(Cn2cc(C(=O)N[C@H]3CCCC[C@@H]3O)c3ncccc32)cc1
CHEMBL2333481 acm1_human Human No 5.8 EC50 = 1800 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
426 4 0 4 4.5 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)cc2)cn1
CHEMBL4756974 acm1_human Human No 6.7 EC50 = 181 nM Funct
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
413 5 1 4 3.6 O=C(NCC1CCCO1)c1cc(Cc2ccc(Br)cc2)c2cccn2n1
CHEMBL4246159 acm1_human Human No 6.7 EC50 = 182.0 nM Funct
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
443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1
CHEMBL4246159 acm1_rat Rat No 6.7 EC50 = 182.0 nM Funct
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
443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1
CHEMBL60479 acm1_human Human No 5.7 EC50 = 1810 nM Funct
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.
393 3 0 5 3.8 Clc1cc(Cl)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1
CHEMBL2333481 acm1_human Human No 5.7 EC50 = 1819.7 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
426 4 0 4 4.5 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)cc2)cn1
CHEMBL4783540 acm1_human Human No 6.7 EC50 = 182 nM Funct
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
415 5 1 6 3.2 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nn4cccc34)cc2)cn1
CHEMBL3618446 acm1_human Human No 6.7 EC50 = 183 nM Funct
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
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
CHEMBL4225919 acm1_human Human No 6.7 EC50 = 184 nM Funct
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
459 6 2 8 2.2 Cn1ccc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@H]4O)c4nc(C=O)ccc43)cc2)n1
CHEMBL4211802 acm1_human Human No 5.7 EC50 = 1846 nM Funct
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
344 2 2 3 4.1 CC(C)(O)C1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S
CHEMBL3746904 acm1_human Human No 6.7 EC50 = 185 nM Funct
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
400 4 2 5 3.7 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc3ncccc3c2)c2cccnc12
CHEMBL1773111 acm1_rat Rat No 5.7 EC50 = 1850 nM Funct
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
511 7 2 7 4.1 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cn[nH]c4)c3)c3cc(F)cc(F)c23)no1
CHEMBL4072818 acm1_human Human Yes 6.7 EC50 = 186.2 nM Bind
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
362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1
CHEMBL4130084 acm1_human Human No 6.7 EC50 = 186.2 nM Funct
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
434 5 2 7 1.9 O=C(N[C@H]1CCOC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL965 acm1_human Human Yes 4.7 EC50 = 18620.9 nM Bind
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
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL4203218 acm1_human Human No 6.7 EC50 = 187 nM Funct
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
314 2 1 2 4.7 CC[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S
CHEMBL1243328 acm1_human Human No 7.7 EC50 = 19 nM Funct
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
361 6 1 3 2.5 CCC(=O)NC1CCN(CCCN2C(=O)CCc3c(F)cccc32)CC1
CHEMBL1083926 acm1_human Human No 7.7 EC50 = 20.0 nM Funct
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
360 4 2 2 4.1 C[C@H]1CNCC[C@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1
CHEMBL1084993 acm1_human Human No 7.7 EC50 = 20.0 nM Funct
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
342 4 2 2 4.0 CC1CNCCC1CNC(=O)c1ccccc1-c1cccc(Cl)c1
CHEMBL4130084 acm1_human Human No 6.7 EC50 = 190 nM Funct
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
434 5 2 7 1.9 O=C(N[C@H]1CCOC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL3354065 acm1_human Human Yes 6.7 EC50 = 190.6 nM Bind
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
328 7 0 2 4.3 CCCCC1CCN(CC1)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL2024423 acm1_human Human No 5.7 EC50 = 1900 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
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
CHEMBL354738 acm1_human Human No 5.7 EC50 = 1900 nM Funct
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
178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2
CHEMBL3823130 acm1_human Human Yes 5.7 EC50 = 1900 nM Funct
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
322 3 0 4 2.8 Cn1cc(-c2ccc(CN3Cc4ncccc4C3=O)c(F)c2)cn1
CHEMBL4130287 acm1_human Human No 5.7 EC50 = 1900 nM Funct
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
432 7 2 6 2.9 CC(O)(CNC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1)C1CC1
CHEMBL4130287 acm1_human Human No 5.7 EC50 = 1905.5 nM Funct
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
432 7 2 6 2.9 CC(O)(CNC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1)C1CC1
CHEMBL3360949 acm1_human Human No 5.7 EC50 = 1940 nM Funct
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
491 5 0 6 5.6 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-c5cnn(C)c5)cc4F)cc-3c2=O)c(C)c1
CHEMBL3360949 acm1_human Human No 5.7 EC50 = 1949.8 nM Funct
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
491 5 0 6 5.6 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-c5cnn(C)c5)cc4F)cc-3c2=O)c(C)c1
CHEMBL3618441 acm1_human Human No 6.7 EC50 = 198 nM Funct
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
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
CHEMBL1223938 acm1_human Human No 6.7 EC50 = 199.5 nM Funct
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
450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1
CHEMBL216927 acm1_human Human Yes 5.7 EC50 = 1995.3 nM Funct
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
487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1
CHEMBL553058 acm1_human Human Yes 5.7 EC50 = 1995.3 nM Funct
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
487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1
CHEMBL2333477 acm1_human Human No 5.7 EC50 = 1995.3 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
444 4 0 4 4.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)cc2F)cn1
CHEMBL2333875 acm1_human Human Yes 5.7 EC50 = 1995.3 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
379 3 0 5 3.0 Cn1cc(-c2ccc(CN3C(=O)C4(OCCO4)c4ccccc43)c(F)c2)cn1
CHEMBL3121473 acm1_human Human No 8.7 EC50 = 2.0 nM Funct
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
197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C
CHEMBL491209 acm1_human Human Yes 8.7 EC50 = 2.1 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1
CHEMBL92421 acm1_rat Rat Yes 8.6 EC50 = 2.4 nM Funct
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)
179 1 0 4 0.8 Cc1noc(C2CN3CCC2C3)n1
CHEMBL293982 acm1_human Human No 8.6 EC50 = 2.5 nM Funct
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.
343 3 0 5 2.6 Fc1cccc(C#CCSc2nsnc2C23CN4CC2C3C4)c1
CHEMBL1223862 acm1_human Human No 8.6 EC50 = 2.5 nM Funct
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
388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1
CHEMBL1223939 acm1_human Human No 8.6 EC50 = 2.5 nM Funct
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
450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1
CHEMBL1223940 acm1_human Human No 8.6 EC50 = 2.5 nM Funct
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
402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1
CHEMBL2059310 acm1_human Human No 7.7 EC50 = 20 nM Funct
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
405 5 1 5 2.7 O=C1CCc2cccnc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1
CHEMBL1243358 acm1_human Human No 7.7 EC50 = 20 nM Funct
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
361 6 1 3 2.5 CCC(=O)NC1CCN(CCCN2C(=O)CCc3ccc(F)cc32)CC1
CHEMBL1243387 acm1_human Human No 7.7 EC50 = 20 nM Funct
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
379 6 1 3 2.6 CCC(=O)NC1CCN(CCCN2C(=O)CCc3cc(F)c(F)cc32)CC1
CHEMBL4740865 acm1_human Human No 7.7 EC50 = 20 nM Funct
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
422 5 2 7 1.4 Cc1c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCOC[C@@H]2O)c(=O)n1C
CHEMBL291872 acm1_human Human No 7.7 EC50 = 20.2 nM Funct
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.
345 3 0 5 2.1 Fc1cc(F)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1
CHEMBL3354067 acm1_human Human No 7.7 EC50 = 20.4 nM Bind
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
537 12 0 7 5.3 CN1CCC=C(c2nsnc2OCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1
CHEMBL3618440 acm1_human Human No 7.7 EC50 = 20.9 nM Funct
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
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
CHEMBL3084451 acm1_human Human No 6.7 EC50 = 200 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
381 6 2 4 2.2 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cc(F)cc(F)c1
CHEMBL1624037 acm1_rat Rat No 6.7 EC50 = 200 nM Funct
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
333 6 2 4 1.9 CCOC(=O)N1CCC(CC1)NCCNC(=O)C2=CC=CC=C2C
CHEMBL21536 acm1_human Human Yes 6.7 EC50 = 200 nM Funct
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.
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL1535797 acm1_rat Rat Yes 6.7 EC50 = 200 nM Funct
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
319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1
CHEMBL1609153 acm1_rat Rat Yes 6.7 EC50 = 200 nM Funct
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
319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1
CHEMBL3329755 acm1_rat Rat Yes 5.7 EC50 = 2000 nM Funct
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
494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F
CHEMBL2022944 acm1_human Human No 5.7 EC50 = 2000 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
354 5 2 5 0.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)N1CCOCC1)C2
CHEMBL2024410 acm1_human Human No 5.7 EC50 = 2000 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
357 7 2 4 2.3 C=CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1)C2
CHEMBL2315678 acm1_rat Rat No 5.7 EC50 = 2000 nM Funct
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
437 4 1 4 3.3 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(Br)c3)C2)CC1
CHEMBL2333477 acm1_human Human No 5.7 EC50 = 2000 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
444 4 0 4 4.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)cc2F)cn1
CHEMBL2333875 acm1_human Human Yes 5.7 EC50 = 2000 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
379 3 0 5 3.0 Cn1cc(-c2ccc(CN3C(=O)C4(OCCO4)c4ccccc43)c(F)c2)cn1
CHEMBL667 acm1_human Human Yes 4.7 EC50 = 20000 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL3360940 acm1_human Human No 5.7 EC50 = 2020 nM Funct
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
411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(F)cc4)cc-3c2=O)c(C)c1
CHEMBL3354073 acm1_human Human No 6.7 EC50 = 204.2 nM Bind
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
358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1
CHEMBL2315678 acm1_rat Rat No 5.7 EC50 = 2041.7 nM Funct
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
437 4 1 4 3.3 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(Br)c3)C2)CC1
CHEMBL3360940 acm1_human Human No 5.7 EC50 = 2041.7 nM Funct
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
411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(F)cc4)cc-3c2=O)c(C)c1
CHEMBL4754262 acm1_human Human No 6.7 EC50 = 208 nM Funct
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
391 5 2 5 2.7 Cc1ccc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1
CHEMBL151938 acm1_human Human Yes 7.7 EC50 = 21 nM Funct
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
154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C
CHEMBL2024407 acm1_human Human No 6.7 EC50 = 210 nM Funct
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](NCCNC(=O)c1ccccc1)C2
CHEMBL1242950 acm1_human Human Yes 6.7 EC50 = 210 nM Funct
Partial agonist activity at EGFP-fused human full length M1 receptor expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayPartial agonist activity at EGFP-fused human full length M1 receptor expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C
CHEMBL4238861 acm1_human Human No 6.7 EC50 = 210 nM Bind
Positive allosteric modulation of M1 AchR (unknown origin)Positive allosteric modulation of M1 AchR (unknown origin)
465 5 2 6 3.8 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCCC[C@@H]4O)c4c(F)cc(F)cc43)cn2)cn1
CHEMBL4229203 acm1_human Human Yes 6.7 EC50 = 210 nM Funct
Positive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization preincubated for 2.5 mins followed by acetylcholine addition measured after 1 min by Fluo-4AM-based FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization preincubated for 2.5 mins followed by acetylcholine addition measured after 1 min by Fluo-4AM-based FLIPR assay
465 5 2 6 3.8 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@@H]4CCCC[C@H]4O)c4c(F)cc(F)cc43)cn2)cn1
CHEMBL2024329 acm1_human Human No 5.7 EC50 = 2100 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@H](NC(=O)c3ccccc3C)C1)C2
CHEMBL485913 acm1_human Human No 5.7 EC50 = 2100 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1
CHEMBL143434 acm1_human Human No 5.7 EC50 = 2100 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
564 15 0 10 6.8 CN1CCC=C(c2nsnc2SCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1
CHEMBL4127506 acm1_human Human No 5.7 EC50 = 2100 nM Funct
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
431 5 2 5 3.7 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccc3)cc2)c2ccccc2O1
CHEMBL3747004 acm1_human Human No 6.7 EC50 = 211 nM Funct
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
445 5 2 7 2.7 Cc1cnc2c(C(=O)N[C@H]3CCOC[C@@H]3O)cn(Cc3ccc(-c4ccn(C)n4)cc3)c2c1
CHEMBL471636 acm1_human Human No 5.7 EC50 = 2110 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
452 3 1 4 4.2 Cc1cccc(C(=O)N2CCC(N3CCC(n4c(=O)[nH]c5cc(Cl)ccc54)CC3)CC2)c1
CHEMBL4130246 acm1_human Human No 5.7 EC50 = 2138.0 nM Funct
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
446 6 2 6 2.7 O=C(NCC(O)C(F)(F)F)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL3746104 acm1_human Human No 6.7 EC50 = 215 nM Funct
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
416 5 2 7 2.7 O=C(N[C@H]1CCCC[C@@H]1O)c1nn(Cc2ccc(-n3cccn3)cc2)c2cccnc12
CHEMBL4214189 acm1_human Human No 5.7 EC50 = 2154 nM Funct
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
396 1 1 2 4.0 Fc1ccccc1C1=NCC(=S)Nc2ccc(I)cc21
CHEMBL4212760 acm1_rat Rat No 6.7 EC50 = 218 nM Funct
Positive allosteric modulation of rat M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of rat M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
346 2 1 2 5.1 CC(C)[C@@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S
CHEMBL4127356 acm1_human Human No 5.7 EC50 = 2187.8 nM Funct
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
450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccc(F)cc2O1
CHEMBL1255785 acm1_rat Rat Yes 6.7 EC50 = 219 nM Funct
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O
CHEMBL12587 acm1_rat Rat Yes 6.7 EC50 = 219 nM Funct
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O
CHEMBL292911 acm1_rat Rat Yes 6.7 EC50 = 219 nM Funct
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O
CHEMBL1773100 acm1_rat Rat No 5.7 EC50 = 2190 nM Funct
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
475 7 2 7 3.8 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cn[nH]c4)c3)c3ccccc23)no1
CHEMBL433867 acm1_human Human No 7.7 EC50 = 22.3 nM Funct
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.
299 6 0 6 2.9 CCCCSc1nsnc1OC1CN2CCC1CC2
CHEMBL3616501 acm1_human Human No 7.6 EC50 = 22.8 nM Funct
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
507 6 2 3 6.1 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(-c3ccccc3)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1
CHEMBL4128022 acm1_human Human No 6.7 EC50 = 220 nM Funct
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
447 5 2 7 2.7 Cn1cc(-c2ccc(CN3CC(C(=O)N[C@H]4CCCC[C@@H]4O)Oc4ccccc43)cn2)cn1
CHEMBL2024406 acm1_human Human No 5.7 EC50 = 2200 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
357 4 1 4 2.3 CCOC(=O)N1C2CCC1CC(N1CC(NC(=O)c3ccccc3)C1)C2
CHEMBL4127356 acm1_human Human No 5.7 EC50 = 2200 nM Funct
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
450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccc(F)cc2O1
CHEMBL4130246 acm1_human Human No 5.7 EC50 = 2200 nM Funct
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
446 6 2 6 2.7 O=C(NCC(O)C(F)(F)F)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL4248057 acm1_rat Rat No 5.7 EC50 = 2238.7 nM Funct
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
445 5 2 7 2.4 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cc2)n1
CHEMBL4126393 acm1_human Human No 5.7 EC50 = 2238.7 nM Funct
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
431 5 2 6 3.0 NC1CCCCC1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL4127046 acm1_human Human No 5.7 EC50 = 2238.7 nM Funct
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
407 5 2 5 3.1 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(C3CC3)nc2)c2ccccc2O1
CHEMBL4800374 acm1_human Human No 6.7 EC50 = 224 nM Funct
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
460 5 2 5 4.7 O=C(N[C@H]1CCCC[C@@H]1O)c1cc(Cc2ccc(-c3ccnc(Cl)c3)cc2)c2cccn2n1
CHEMBL4248057 acm1_rat Rat No 5.7 EC50 = 2240 nM Funct
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
445 5 2 7 2.4 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cc2)n1
CHEMBL126237 acm1_human Human No 6.7 EC50 = 225 nM Funct
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.
327 8 0 6 3.7 CCCCCCSc1nsnc1OC1CN2CCC1CC2
CHEMBL3354074 acm1_human Human No 6.6 EC50 = 229.1 nM Bind
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
386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1
CHEMBL4238059 acm1_rat Rat Yes 6.6 EC50 = 229.1 nM Funct
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
430 5 1 7 2.9 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cn2)cn1
CHEMBL4240517 acm1_rat Rat No 5.6 EC50 = 2290 nM Funct
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
444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1
CHEMBL4240517 acm1_rat Rat No 5.6 EC50 = 2290.9 nM Funct
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
444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1
CHEMBL4127312 acm1_human Human No 5.6 EC50 = 2290.9 nM Funct
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
429 5 1 6 3.8 O=C(Nc1ncccc1F)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL64000 acm1_rat Rat Yes 7.6 EC50 = 23 nM Funct
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2
CHEMBL4085548 acm1_human Human No 7.6 EC50 = 23 nM Funct
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
432 4 1 5 3.7 Cc1nc(-c2ccc(Cc3cc4c(cc3C)CCN([C@H]3CCOC[C@@H]3O)C4=O)cc2)co1
CHEMBL4238059 acm1_rat Rat Yes 6.6 EC50 = 230 nM Funct
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
430 5 1 7 2.9 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cn2)cn1
CHEMBL2024419 acm1_human Human No 5.6 EC50 = 2300 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
379 6 2 4 2.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1Cl)C2
CHEMBL1624037 acm1_human Human No 5.6 EC50 = 2300 nM Funct
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
333 6 2 4 1.9 CCOC(=O)N1CCC(CC1)NCCNC(=O)C2=CC=CC=C2C
CHEMBL485755 acm1_human Human No 5.6 EC50 = 2300 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
458 4 1 5 3.0 O=c1[nH]c2cc(F)ccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1
CHEMBL1624037 acm1_rat Rat No 5.6 EC50 = 2300 nM Funct
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
333 6 2 4 1.9 CCOC(=O)N1CCC(CC1)NCCNC(=O)C2=CC=CC=C2C
CHEMBL4126393 acm1_human Human No 5.6 EC50 = 2300 nM Funct
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
431 5 2 6 3.0 NC1CCCCC1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL4127312 acm1_human Human No 5.6 EC50 = 2300 nM Funct
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
429 5 1 6 3.8 O=C(Nc1ncccc1F)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL1083205 acm1_human Human No 5.6 EC50 = 2300 nM Funct
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
353 3 0 4 3.1 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1
CHEMBL1084941 acm1_human Human No 5.6 EC50 = 2300 nM Funct
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
317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1
CHEMBL4207635 acm1_human Human No 6.6 EC50 = 232 nM Funct
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
378 3 1 3 5.2 CC(C)[C@@H]1N=C(c2ccccc2)c2cc(OC(F)(F)F)ccc2NC1=S
CHEMBL1083205 acm1_rat Rat No 5.6 EC50 = 2320 nM Funct
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])]
353 3 0 4 3.1 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1
CHEMBL4214867 acm1_human Human No 6.6 EC50 = 238 nM Funct
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
328 3 1 2 5.1 CCC[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S
CHEMBL2313520 acm1_human Human No 5.6 EC50 = 2398.8 nM Funct
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
321 3 0 3 3.3 Cn1cc(-c2ccc(CN3C(=O)Cc4ccccc43)c(F)c2)cn1
CHEMBL4072572 acm1_human Human No 7.6 EC50 = 24 nM Funct
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
420 4 1 5 3.8 Cc1cc2c(cc1Cc1ccc(-c3cscn3)cc1)C(=O)N([C@H]1CCOC[C@@H]1O)C2
CHEMBL3084450 acm1_human Human No 6.6 EC50 = 240 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
375 7 2 5 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccc(OC)c1
CHEMBL2313520 acm1_human Human No 5.6 EC50 = 2400 nM Funct
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
321 3 0 3 3.3 Cn1cc(-c2ccc(CN3C(=O)Cc4ccccc43)c(F)c2)cn1
CHEMBL1084941 acm1_rat Rat No 5.6 EC50 = 2420 nM Funct
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])]
317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1
CHEMBL3360958 acm1_human Human No 5.6 EC50 = 2430 nM Funct
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
355 3 0 6 3.1 Cn1nc2c3ccccc3n(Cc3ccc(-n4cccn4)cc3)cc-2c1=O
CHEMBL2333472 acm1_human Human No 5.6 EC50 = 2454.7 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
454 4 0 6 3.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(c5ncccn5)C4)c4ccccc43)c(F)c2)cn1
CHEMBL3745855 acm1_human Human No 6.6 EC50 = 248 nM Funct
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
429 6 2 6 3.6 O=C(N[C@H]1CC[C@H](CO)CC1)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12
CHEMBL1083621 acm1_human Human No 7.6 EC50 = 25.1 nM Funct
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
380 4 2 2 4.5 O=C(NCC1CCNCC1)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F
CHEMBL1084818 acm1_human Human No 7.6 EC50 = 25.1 nM Funct
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
346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1ccc(F)c(Cl)c1
CHEMBL1223807 acm1_human Human No 7.6 EC50 = 25.1 nM Funct
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
358 4 0 5 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccccc43)CC2)CC1
CHEMBL3608415 acm1_human Human No 7.6 EC50 = 25.3 nM Funct
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
448 5 2 7 3.1 Cn1cc(-c2ccc(Cn3nc(C(=O)N[C@H]4CCCC[C@@H]4O)c4ncccc43)c(F)c2)cn1
CHEMBL667 acm1_human Human Yes 7.6 EC50 = 25.9 nM Funct
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
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL965 acm1_human Human Yes 6.6 EC50 = 250 nM Funct
Agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL1916228 acm1_rat Rat No 6.6 EC50 = 250 nM Funct
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
389 5 1 5 2.5 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(OC)c3)C2)CC1
CHEMBL4127762 acm1_human Human Yes 6.6 EC50 = 250 nM Funct
Positive allosteric modulation of human muscarinic acetylcholine M1 receptorPositive allosteric modulation of human muscarinic acetylcholine M1 receptor
432 5 2 6 3.1 O=C(N[C@H]1CCCC[C@@H]1O)[C@H]1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL4127762 acm1_rat Rat Yes 6.6 EC50 = 250 nM Funct
Positive allosteric modulation of rat muscarinic acetylcholine M1 receptorPositive allosteric modulation of rat muscarinic acetylcholine M1 receptor
432 5 2 6 3.1 O=C(N[C@H]1CCCC[C@@H]1O)[C@H]1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL2024427 acm1_human Human No 5.6 EC50 = 2500 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
380 5 2 4 2.7 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)N1[C@@H](C)CCC[C@H]1C)C2
CHEMBL2333472 acm1_human Human No 5.6 EC50 = 2500 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
454 4 0 6 3.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(c5ncccn5)C4)c4ccccc43)c(F)c2)cn1
CHEMBL4127046 acm1_human Human No 5.6 EC50 = 2500 nM Funct
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
407 5 2 5 3.1 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(C3CC3)nc2)c2ccccc2O1
CHEMBL1624037 acm1_rat Rat No 4.6 EC50 = 25070 nM Bind
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 ]
333 6 2 4 1.9 CCOC(=O)N1CCC(CC1)NCCNC(=O)C2=CC=CC=C2C
CHEMBL4210455 acm1_human Human No 6.6 EC50 = 251 nM Funct
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
340 3 1 2 5.1 S=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@H]1CC1CC1
CHEMBL216927 acm1_human Human Yes 6.6 EC50 = 251.2 nM Funct
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
487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1
CHEMBL553058 acm1_human Human Yes 6.6 EC50 = 251.2 nM Funct
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
487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1
CHEMBL216928 acm1_human Human No 6.6 EC50 = 251.2 nM Funct
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
487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1
CHEMBL386983 acm1_human Human No 6.6 EC50 = 251.2 nM Funct
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
531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1
CHEMBL1082341 acm1_human Human No 6.6 EC50 = 251.2 nM Funct
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
361 4 1 4 3.7 O=C(NCC12CCN(CC1)CC2)c1ccccc1-c1nc(Cl)cs1
CHEMBL1083911 acm1_human Human No 6.6 EC50 = 251.2 nM Funct
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
335 4 2 4 3.2 O=C(NCC1CCNCC1)c1ccccc1-c1nc(Cl)cs1
CHEMBL1189471 acm1_human Human No 5.6 EC50 = 2511.9 nM Bind
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
423 15 0 7 5.1 CC(=O)OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1
CHEMBL538793 acm1_human Human No 5.6 EC50 = 2511.9 nM Bind
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
423 15 0 7 5.1 CC(=O)OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1
CHEMBL2206333 acm1_human Human No 4.6 EC50 = 25118.9 nM Bind
Displacement of [3H]NMS from EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as reduction of [3H]NMS dissociation rate after 22 hrs by liquid scintillation countingDisplacement of [3H]NMS from EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as reduction of [3H]NMS dissociation rate after 22 hrs by liquid scintillation counting
870 20 1 9 8.3 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCCCCC4CCN(CCCC(=O)c5ccccc5C)CC4)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1
CHEMBL522460 acm1_human Human Yes 6.6 EC50 = 255 nM Funct
Partial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium response
404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1
CHEMBL3745724 acm1_human Human No 6.6 EC50 = 255 nM Funct
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
445 5 2 7 2.7 Cc1ccc2c(n1)c(C(=O)N[C@H]1CCOC[C@@H]1O)cn2Cc1ccc(-c2ccn(C)n2)cc1
CHEMBL522460 acm1_human Human Yes 6.6 EC50 = 257.0 nM Funct
Partial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium response
404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1
CHEMBL4245556 acm1_rat Rat No 6.6 EC50 = 257.0 nM Funct
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
430 5 2 7 2.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCC[C@H]4O)nc4c3ccn4C)cn2)n1
CHEMBL3747724 acm1_human Human No 6.6 EC50 = 258 nM Funct
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
397 5 1 7 3.3 Cn1ccc(NC(=O)c2cn(Cc3ccc(-n4cccn4)cc3)c3cccnc23)n1
CHEMBL126332 acm1_human Human No 6.6 EC50 = 258.9 nM Funct
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.
311 8 0 6 3.0 CCCCCCOc1nsnc1OC1CN2CCC1CC2
CHEMBL4088940 acm1_human Human No 7.6 EC50 = 26 nM Funct
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
418 4 1 5 3.4 Cc1cc2c(cc1Cc1ccc(-c3cocn3)cc1)C(=O)N([C@H]1CCOC[C@@H]1O)CC2
CHEMBL477821 acm1_human Human No 6.6 EC50 = 260 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
424 4 1 4 4.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3Cl)CC2)CC1
CHEMBL4245556 acm1_rat Rat No 6.6 EC50 = 260 nM Funct
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
430 5 2 7 2.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCC[C@H]4O)nc4c3ccn4C)cn2)n1
CHEMBL1624037 acm1_human Human No 5.6 EC50 = 2600 nM Funct
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
333 6 2 4 1.9 CCOC(=O)N1CCC(CC1)NCCNC(=O)C2=CC=CC=C2C
CHEMBL486758 acm1_human Human No 5.6 EC50 = 2600 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
458 4 1 5 3.0 O=c1[nH]c2c(F)cccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1
CHEMBL1916234 acm1_rat Rat No 5.6 EC50 = 2600 nM Funct
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
393 4 1 4 3.2 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3Cl)C2)CC1
CHEMBL21536 acm1_human Human Yes 5.6 EC50 = 2600 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cellsAgonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL3823130 acm1_human Human Yes 5.6 EC50 = 2600 nM Bind
Positive allosteric modulation at human muscarinic acetylcholine receptor M1 assessed as effect on beta-arrestin recruitmentPositive allosteric modulation at human muscarinic acetylcholine receptor M1 assessed as effect on beta-arrestin recruitment
322 3 0 4 2.8 Cn1cc(-c2ccc(CN3Cc4ncccc4C3=O)c(F)c2)cn1
CHEMBL2333478 acm1_human Human No 5.6 EC50 = 2600 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
462 4 0 4 4.8 Cn1cc(-c2cc(F)c(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)c(F)c2)cn1
CHEMBL3354065 acm1_human Human Yes 6.6 EC50 = 263.0 nM Bind
Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on xanomeline-induced response by BRET based Gq protein activation assayPositive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on xanomeline-induced response by BRET based Gq protein activation assay
328 7 0 2 4.3 CCCCC1CCN(CC1)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL2333478 acm1_human Human No 5.6 EC50 = 2630.3 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
462 4 0 4 4.8 Cn1cc(-c2cc(F)c(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)c(F)c2)cn1
CHEMBL4125860 acm1_human Human No 5.6 EC50 = 2630.3 nM Funct
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
430 5 1 6 3.3 O=C(N[C@H]1CCCCC1=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL4206066 acm1_human Human No 6.6 EC50 = 267 nM Funct
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
344 2 1 2 5.0 CC(C)C1C(=O)N(c2ccccc2)c2cc(Cl)ccc2NC1=S
CHEMBL1243232 acm1_human Human No 7.6 EC50 = 27 nM Funct
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
345 6 1 4 1.8 CCC(=O)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1
CHEMBL4088915 acm1_human Human No 7.6 EC50 = 27 nM Funct
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
417 4 1 5 3.1 Cc1cc2c(cc1Cc1ccc(-c3cnn(C)c3)cc1)C(=O)N([C@H]1CCOC[C@@H]1O)C2
CHEMBL596508 acm1_human Human No 6.6 EC50 = 270 nM Bind
Positive allosteric modulation activity at muscarinic M1 receptorPositive allosteric modulation activity at muscarinic M1 receptor
391 4 1 3 4.7 O=C(O)c1cn(Cc2ccc(-c3ccccc3)cc2)c2c(F)ccc(F)c2c1=O
CHEMBL7634 acm1_mouse Mouse Yes 6.6 EC50 = 270 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1
CHEMBL4125860 acm1_human Human No 5.6 EC50 = 2700 nM Funct
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
430 5 1 6 3.3 O=C(N[C@H]1CCCCC1=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL667 acm1_human Human Yes 4.6 EC50 = 27000 nM Funct
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL667 acm1_human Human Yes 4.6 EC50 = 27000 nM Funct
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
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL167438 acm1_human Human No 4.6 EC50 = 27000 nM Funct
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
168 3 0 3 1.1 CCCO/N=C1\CN2CCC1C2
CHEMBL7303 acm1_mouse Mouse Yes 4.6 EC50 = 27000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C
CHEMBL471635 acm1_human Human No 5.6 EC50 = 2710 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
452 3 1 4 4.2 Cc1ccccc1C(=O)N1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1
CHEMBL3747037 acm1_human Human No 6.6 EC50 = 273 nM Funct
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
492 6 2 7 4.4 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cc(-c4ccncc4)cn3)cc2)c2cccnc12
CHEMBL4211618 acm1_human Human No 6.6 EC50 = 275 nM Funct
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
329 2 1 3 4.4 CC(C)[C@@H]1N=C(c2cccnc2)c2cc(Cl)ccc2NC1=S
CHEMBL3824114 acm1_rat Rat No 5.6 EC50 = 2754.2 nM Funct
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
403 3 0 6 3.7 Cn1cc2cc(-c3cc(F)c(Cn4c(=O)cnc5ncccc54)c(F)c3)ccc2n1
CHEMBL2164910 acm1_human Human No 7.6 EC50 = 28.2 nM Funct
Antagonist activity at human muscarinic M1 receptorAntagonist activity at human muscarinic M1 receptor
326 4 0 2 2.9 CN1CCN(C(=O)C(F)(Cc2ccccc2)c2ccccc2)CC1
CHEMBL319109 acm1_human Human No 7.6 EC50 = 28.3 nM Funct
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@@H]1CN2CCC[C@H]1C2
CHEMBL3608414 acm1_human Human No 7.5 EC50 = 28.5 nM Funct
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
449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@H]4O)c4ncccc43)c(F)c2)cn1
CHEMBL3824114 acm1_rat Rat No 5.6 EC50 = 2800 nM Funct
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
403 3 0 6 3.7 Cn1cc2cc(-c3cc(F)c(Cn4c(=O)cnc5ncccc54)c(F)c3)ccc2n1
CHEMBL4130215 acm1_human Human No 5.6 EC50 = 2800 nM Funct
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
466 5 2 6 3.7 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cc(Cl)ccc2O1
CHEMBL4128093 acm1_human Human No 6.6 EC50 = 281.8 nM Funct
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
433 5 2 7 2.5 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3ccnc3)nc2)c2ccccc2O1
CHEMBL2333865 acm1_human Human Yes 5.5 EC50 = 2884.0 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
390 3 0 4 3.3 CN1CCC2(C1)C(=O)N(Cc1ccc(-c3cnn(C)c3)cc1F)c1ccccc12
CHEMBL522460 acm1_human Human Yes 6.5 EC50 = 289 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1
CHEMBL4216319 acm1_human Human No 6.5 EC50 = 289 nM Funct
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
329 2 1 3 4.4 CC(C)[C@@H]1N=C(c2ccccn2)c2cc(Cl)ccc2NC1=S
CHEMBL4226889 acm1_human Human No 7.5 EC50 = 29 nM Funct
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
420 5 2 6 2.5 Cc1c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C
CHEMBL4226889 acm1_human Human No 7.5 EC50 = 29 nM Funct
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
420 5 2 6 2.5 Cc1c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C
CHEMBL1243074 acm1_human Human No 6.5 EC50 = 290 nM Funct
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
423 7 1 3 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3cccc(F)c32)CC1
CHEMBL335542 acm1_human Human No 6.5 EC50 = 290 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cellsAgonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells
552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1
CHEMBL4128093 acm1_human Human No 6.5 EC50 = 290 nM Funct
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
433 5 2 7 2.5 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3ccnc3)nc2)c2ccccc2O1
CHEMBL2333865 acm1_human Human Yes 5.5 EC50 = 2900 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
390 3 0 4 3.3 CN1CCC2(C1)C(=O)N(Cc1ccc(-c3cnn(C)c3)cc1F)c1ccccc12
CHEMBL1482157 acm1_rat Rat Yes 4.5 EC50 = 29090 nM Bind
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 ]
353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1
CHEMBL3745724 acm1_human Human No 6.5 EC50 = 293 nM Funct
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
445 5 2 7 2.7 Cc1ccc2c(n1)c(C(=O)N[C@H]1CCOC[C@@H]1O)cn2Cc1ccc(-c2ccn(C)n2)cc1
CHEMBL3354075 acm1_human Human No 6.5 EC50 = 295.1 nM Bind
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
414 13 1 3 5.2 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCCCO)CC1
CHEMBL1083618 acm1_human Human No 8.5 EC50 = 3.2 nM Funct
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
344 4 2 2 3.8 O=C(NCC1=CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1
CHEMBL1223805 acm1_human Human No 8.5 EC50 = 3.2 nM Funct
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
356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1
CHEMBL1223863 acm1_human Human No 8.5 EC50 = 3.2 nM Funct
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
383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1
CHEMBL3608417 acm1_human Human No 7.5 EC50 = 30.3 nM Funct
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
449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)c(F)c2)cn1
CHEMBL2059320 acm1_human Human No 6.5 EC50 = 300 nM Funct
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
422 5 1 4 3.5 O=C1CCc2cccc(F)c2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1
CHEMBL2333473 acm1_human Human No 5.5 EC50 = 3000 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
458 4 0 4 5.0 Cc1nn(C)cc1-c1ccc(CN2C(=O)C3(CCN(C4CCCC4)C3)c3ccccc32)c(F)c1
CHEMBL2333473 acm1_human Human No 5.5 EC50 = 3020.0 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
458 4 0 4 5.0 Cc1nn(C)cc1-c1ccc(CN2C(=O)C3(CCN(C4CCCC4)C3)c3ccccc32)c(F)c1
CHEMBL3414843 acm1_human Human No 6.5 EC50 = 302 nM Funct
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
595 12 1 6 5.0 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Cl)c(F)cc2c1=O
CHEMBL3559130 acm1_human Human No 6.5 EC50 = 302 nM Funct
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
595 12 1 6 5.0 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Cl)c(F)cc2c1=O
CHEMBL1773115 acm1_rat Rat No 5.5 EC50 = 3070 nM Funct
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
493 7 2 7 3.9 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cc(-c4cn[nH]c4)ccc3F)c3ccccc23)no1
CHEMBL4130089 acm1_human Human No 6.5 EC50 = 309.0 nM Funct
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
450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cc(F)ccc2O1
CHEMBL2333871 acm1_human Human No 5.5 EC50 = 3090.3 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
444 4 0 4 4.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)c(F)c2)cn1
CHEMBL4126120 acm1_human Human No 5.5 EC50 = 3090.3 nM Funct
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
450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2c(F)cccc2O1
CHEMBL3402921 acm1_human Human No 7.5 EC50 = 31 nM Funct
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
249 2 0 4 1.0 CN1CCC=C(C2=NOC(N3CCCC3=O)C2)C1
CHEMBL3618450 acm1_human Human No 7.5 EC50 = 31 nM Funct
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
465 5 2 3 5.0 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Cl)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1
CHEMBL1083404 acm1_human Human No 7.5 EC50 = 31.6 nM Funct
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
380 4 2 2 4.5 O=C(NCC1CCNCC1)c1c(F)cccc1-c1cc(Cl)ccc1Cl
CHEMBL594432 acm1_human Human No 7.5 EC50 = 31.6 nM Funct
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
345 4 1 4 3.0 COc1ccc(Cn2cc(C(=O)O)c(=O)c3c(F)ccc(F)c32)cc1
CHEMBL1243386 acm1_human Human No 6.5 EC50 = 310 nM Funct
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
361 6 1 3 2.5 CCC(=O)NC1CCN(CCCN2C(=O)CCc3cccc(F)c32)CC1
CHEMBL1916229 acm1_rat Rat No 6.5 EC50 = 310 nM Funct
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
395 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccc(F)c(F)c3)C2)CC1
CHEMBL3360927 acm1_human Human No 6.5 EC50 = 310 nM Bind
Positive allosteric modulation of M1 AchR (unknown origin)Positive allosteric modulation of M1 AchR (unknown origin)
526 7 1 9 3.5 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3ccc(-c4cnn(C)c4)nc3)c3cc(F)cc(F)c23)no1
CHEMBL2333871 acm1_human Human No 5.5 EC50 = 3100 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
444 4 0 4 4.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)c(F)c2)cn1
CHEMBL4215404 acm1_human Human No 6.5 EC50 = 311 nM Funct
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
368 2 1 2 5.3 FC(F)(F)C[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S
CHEMBL3290084 acm1_human Human No 6.5 EC50 = 316.2 nM Bind
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
361 4 1 5 2.4 O=C(O)c1cn(Cc2ccc(S(=O)(=O)F)cc2)c2ccccc2c1=O
CHEMBL21536 acm1_human Human Yes 6.5 EC50 = 316.2 nM Funct
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
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL376295 acm1_human Human No 5.5 EC50 = 3162.3 nM Funct
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
467 16 0 12 3.1 COc1nsnc1OCCCOCCCOCCCOc1nsnc1-c1cccnc1
CHEMBL1086298 acm1_human Human No 5.5 EC50 = 3162.3 nM Funct
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
342 5 2 2 4.1 O=C(NCCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1
CHEMBL965 acm1_human Human Yes 5.5 EC50 = 3162.3 nM Bind
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
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL1193635 acm1_human Human No 5.5 EC50 = 3162.3 nM Bind
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
381 14 1 6 4.5 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCO)C1
CHEMBL545077 acm1_human Human No 5.5 EC50 = 3162.3 nM Bind
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
381 14 1 6 4.5 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCO)C1
CHEMBL4209299 acm1_human Human No 6.5 EC50 = 317 nM Funct
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
303 1 1 1 5.1 Fc1ccccc1C1=CCC(=S)Nc2ccc(Cl)cc21
CHEMBL4210984 acm1_human Human No 6.5 EC50 = 317 nM Funct
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
342 3 1 2 5.3 CC(C)C[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S
CHEMBL4218941 acm1_human Human Yes 6.5 EC50 = 317 nM Funct
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
304 1 1 2 4.1 Fc1ccccc1C1=NCC(=S)Nc2ccc(Cl)cc21
CHEMBL4126120 acm1_human Human No 5.5 EC50 = 3180 nM Funct
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
450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2c(F)cccc2O1
CHEMBL3414840 acm1_human Human No 7.5 EC50 = 32.4 nM Funct
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
567 10 1 6 4.2 C[N+](C)(CC#CCOC1=NOCC1)CCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Cl)c(F)cc2c1=O
CHEMBL3559070 acm1_human Human No 7.5 EC50 = 32.4 nM Funct
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
567 10 1 6 4.2 C[N+](C)(CC#CCOC1=NOCC1)CCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Cl)c(F)cc2c1=O
CHEMBL2024405 acm1_human Human No 6.5 EC50 = 320 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
371 4 1 4 2.6 CCOC(=O)N1C2CCC1CC(N1CC[C@@H](NC(=O)c3ccccc3)C1)C2
CHEMBL4238059 acm1_human Human Yes 6.5 EC50 = 320 nM Funct
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
430 5 1 7 2.9 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cn2)cn1
CHEMBL4130089 acm1_human Human No 6.5 EC50 = 320 nM Funct
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
450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cc(F)ccc2O1
CHEMBL503735 acm1_rat Rat Yes 5.5 EC50 = 3200 nM Funct
Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21
CHEMBL2024327 acm1_human Human No 5.5 EC50 = 3200 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
359 5 1 4 2.4 CCOC(=O)N1CC[C@H]2[C@@H](CCCN2CCNC(=O)c2ccccc2)C1
CHEMBL503735 acm1_rat Rat Yes 5.5 EC50 = 3200 nM Funct
Agonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilization
339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21
CHEMBL7303 acm1_human Human Yes 5.5 EC50 = 3200 nM Bind
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)
155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C
CHEMBL2333875 acm1_human Human Yes 5.5 EC50 = 3200 nM Bind
Positive allosteric modulation at muscarinic acetylcholine receptor M1(unknown origin)Positive allosteric modulation at muscarinic acetylcholine receptor M1(unknown origin)
379 3 0 5 3.0 Cn1cc(-c2ccc(CN3C(=O)C4(OCCO4)c4ccccc43)c(F)c2)cn1
CHEMBL3823130 acm1_rat Rat Yes 5.5 EC50 = 3200 nM Funct
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
322 3 0 4 2.8 Cn1cc(-c2ccc(CN3Cc4ncccc4C3=O)c(F)c2)cn1
CHEMBL2333482 acm1_human Human No 5.5 EC50 = 3200 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
404 4 0 4 3.7 CCN1CCC2(C1)C(=O)N(Cc1ccc(-c3cnn(C)c3)cc1F)c1ccccc12
CHEMBL2333865 acm1_human Human Yes 5.5 EC50 = 3200 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
390 3 0 4 3.3 CN1CCC2(C1)C(=O)N(Cc1ccc(-c3cnn(C)c3)cc1F)c1ccccc12
CHEMBL2313515 acm1_human Human No 5.5 EC50 = 3200 nM Funct
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
353 3 0 4 3.9 Cn1cc(-c2ccc(CN3C(=O)CSc4ccccc43)c(F)c2)cn1
CHEMBL1773099 acm1_rat Rat No 5.5 EC50 = 3210 nM Funct
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
489 7 1 8 3.8 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cnn(C)c4)c3)c3ccccc23)no1
CHEMBL4238059 acm1_human Human Yes 6.5 EC50 = 323.6 nM Funct
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
430 5 1 7 2.9 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cn2)cn1
CHEMBL4246159 acm1_rat Rat No 5.5 EC50 = 3235.9 nM Funct
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
443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1
CHEMBL2333482 acm1_human Human No 5.5 EC50 = 3235.9 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
404 4 0 4 3.7 CCN1CCC2(C1)C(=O)N(Cc1ccc(-c3cnn(C)c3)cc1F)c1ccccc12
CHEMBL2333865 acm1_human Human Yes 5.5 EC50 = 3235.9 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
390 3 0 4 3.3 CN1CCC2(C1)C(=O)N(Cc1ccc(-c3cnn(C)c3)cc1F)c1ccccc12
CHEMBL2313515 acm1_human Human No 5.5 EC50 = 3235.9 nM Funct
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
353 3 0 4 3.9 Cn1cc(-c2ccc(CN3C(=O)CSc4ccccc43)c(F)c2)cn1
CHEMBL4246159 acm1_rat Rat No 5.5 EC50 = 3240 nM Funct
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
443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1
CHEMBL485953 acm1_human Human No 5.5 EC50 = 3300 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
458 4 1 5 3.0 O=c1[nH]c2ccc(F)cc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1
CHEMBL84893 acm1_human Human No 5.5 EC50 = 3300 nM Funct
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
240 2 0 3 1.7 C(#Cc1ccccc1)CO/N=C1\CN2CCC1C2
CHEMBL2313498 acm1_human Human No 5.5 EC50 = 3300 nM Funct
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
405 3 1 4 3.5 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1
CHEMBL2313499 acm1_human Human No 5.5 EC50 = 3300 nM Funct
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
419 4 1 4 4.0 CCn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1
CHEMBL1191029 acm1_mouse Mouse Yes 4.5 EC50 = 33000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1
CHEMBL542065 acm1_mouse Mouse Yes 4.5 EC50 = 33000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1
CHEMBL2313498 acm1_human Human No 5.5 EC50 = 3311.3 nM Funct
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
405 3 1 4 3.5 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1
CHEMBL2313499 acm1_human Human No 5.5 EC50 = 3311.3 nM Funct
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
419 4 1 4 4.0 CCn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1
CHEMBL478662 acm1_human Human No 6.5 EC50 = 334 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
458 4 1 4 4.7 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1
CHEMBL965 acm1_human Human Yes 4.5 EC50 = 33500 nM Bind
Activation of M1-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M1-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL4225344 acm1_human Human No 6.5 EC50 = 338 nM Funct
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
408 6 3 7 1.2 O=C(N[C@H]1CCOC[C@@H]1O)c1cc(Cc2ccc(-n3cccn3)cc2)c(CO)cn1
CHEMBL4225950 acm1_human Human No 7.5 EC50 = 34 nM Funct
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
431 5 2 6 3.4 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc([N+]3([O-])C=CC=N3)cc2)c2cccnc12
CHEMBL3608413 acm1_rat Rat No 7.5 EC50 = 34.6 nM Funct
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
447 5 2 6 3.7 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCCC[C@@H]4O)c4ncccc43)c(F)c2)cn1
CHEMBL3354065 acm1_human Human Yes 7.5 EC50 = 34.7 nM Bind
Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on carbachol-induced response by BRET based Gq protein engagement assayPositive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on carbachol-induced response by BRET based Gq protein engagement assay
328 7 0 2 4.3 CCCCC1CCN(CC1)CCCN2C(=O)CCC3=CC=CC=C32
CHEMBL3608420 acm1_human Human No 7.5 EC50 = 34.8 nM Funct
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
432 5 2 8 1.8 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cn2)cn1
CHEMBL142538 acm1_human Human No 6.5 EC50 = 340 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
560 17 0 10 6.2 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1
CHEMBL4757070 acm1_human Human No 6.5 EC50 = 343 nM Funct
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
415 6 1 6 3.2 Cn1cc(-c2ccc(Cc3cc(C(=O)NCC4CCCO4)nn4cccc34)cc2)cn1
CHEMBL1565295 acm1_rat Rat No 5.5 EC50 = 3449 nM Funct
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])]
489 7 1 8 3.8 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4ccn(C)n4)c3)c3ccccc23)no1
CHEMBL4213699 acm1_human Human No 6.5 EC50 = 349 nM Funct
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
344 2 1 2 4.5 CC(C)C1C(=S)Nc2ccc(Cl)cc2C(c2ccccc2)=[N+]1[O-]
CHEMBL2024332 acm1_human Human No 6.5 EC50 = 350 nM Funct
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
385 4 1 4 3.0 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3)C1)C2
CHEMBL1243296 acm1_human Human No 6.5 EC50 = 350 nM Funct
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
385 6 1 4 2.6 O=C(NC1CCN(CCCN2C(=O)COc3ccccc32)CC1)C1CCCC1
CHEMBL337131 acm1_human Human No 6.5 EC50 = 350 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
466 8 0 10 4.1 CN1CCC=C(c2nsnc2SCCCSc2nsnc2C2=CCCN(C)C2)C1
CHEMBL40554 acm1_human Human Yes 5.5 EC50 = 3500 nM Funct
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
281 3 1 2 2.6 C[N+](C)(C)CC#CCOC(=O)NC1=CC(=CC=C1)Cl
CHEMBL3289440 acm1_human Human No 6.5 EC50 = 352 nM Funct
Agonist activity at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as calcium mobilization by FLIPR assay
436 4 0 6 2.1 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(S(C)(=O)=O)c2ncccc23)CC1
CHEMBL4207900 acm1_human Human No 6.5 EC50 = 354 nM Funct
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
344 3 1 3 4.3 COC(C)C1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S
CHEMBL490597 acm1_human Human No 6.5 EC50 = 356 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
424 4 1 4 4.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3)CC2)CC1
CHEMBL3616500 acm1_human Human No 7.4 EC50 = 36 nM Funct
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
499 5 2 3 5.4 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C(F)(F)F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1
CHEMBL4094233 acm1_human Human No 7.4 EC50 = 36 nM Funct
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
403 4 1 5 2.9 Cc1cc2c(cc1Cc1ccc(-n3cccn3)cc1)C(=O)N([C@H]1CCOC[C@@H]1O)C2
CHEMBL4765183 acm1_human Human No 7.4 EC50 = 36 nM Funct
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
469 6 3 6 3.1 NC(=O)c1cncc(-c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)nn4cccc34)cc2)c1
CHEMBL4244259 acm1_rat Rat No 6.4 EC50 = 360 nM Funct
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
446 5 2 6 4.3 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)N[C@@H]3CCCC[C@H]3O)nc21
CHEMBL2024422 acm1_human Human No 5.4 EC50 = 3600 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
375 7 2 5 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cccc(OC)c1)C2
CHEMBL3084454 acm1_human Human No 5.4 EC50 = 3600 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
337 6 2 4 1.7 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)C1CCCC1
CHEMBL487986 acm1_human Human No 5.4 EC50 = 3600 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
553 4 2 5 5.9 O=C(Nc1cccc(SC(F)(F)F)c1)N1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1
CHEMBL4244259 acm1_rat Rat No 6.4 EC50 = 363.1 nM Funct
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
446 5 2 6 4.3 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)N[C@@H]3CCCC[C@H]3O)nc21
CHEMBL4126902 acm1_human Human No 5.4 EC50 = 3630.8 nM Funct
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
435 4 2 5 3.3 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(C(F)(F)F)nc2)c2ccccc2O1
CHEMBL3360945 acm1_human Human No 5.4 EC50 = 3630.8 nM Funct
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
394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccnc4)cc-3c2=O)c(C)c1
CHEMBL1181943 acm1_human Human No 4.4 EC50 = 36307.8 nM Funct
Potency at muscarinic receptor M1 in rabbit vas deferensPotency at muscarinic receptor M1 in rabbit vas deferens
574 13 0 3 4.8 CC(C)(CN1C(=O)c2cccc3cccc(c23)C1=O)C[N+](C)(C)CCCCCC[N+](C)(C)CC#CCN1CCCC1=O
CHEMBL199636 acm1_human Human No 4.4 EC50 = 36307.8 nM Funct
Potency at muscarinic receptor M1 in rabbit vas deferensPotency at muscarinic receptor M1 in rabbit vas deferens
574 13 0 3 4.8 CC(C)(CN1C(=O)c2cccc3cccc(c23)C1=O)C[N+](C)(C)CCCCCC[N+](C)(C)CC#CCN1CCCC1=O
CHEMBL1535797 acm1_rat Rat Yes 4.4 EC50 = 36480 nM Bind
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 ]
319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1
CHEMBL1609153 acm1_rat Rat Yes 4.4 EC50 = 36480 nM Bind
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 ]
319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1
CHEMBL4097569 acm1_human Human Yes 6.4 EC50 = 365 nM Bind
Positive allosteric modulation of muscarinic M1 receptor (unknown origin) assessed as increase in Ach-induced recruitment of beta-arrestin by Path Hunter assayPositive allosteric modulation of muscarinic M1 receptor (unknown origin) assessed as increase in Ach-induced recruitment of beta-arrestin by Path Hunter assay
409 5 2 6 3.0 O[C@H]1COCC[C@@H]1NC(=O)c1ncc(c(c1)Cc1ccc(cc1)c1cscn1)C
CHEMBL3360945 acm1_human Human No 5.4 EC50 = 3660 nM Funct
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
394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccnc4)cc-3c2=O)c(C)c1
CHEMBL4211235 acm1_human Human Yes 5.4 EC50 = 3678 nM Funct
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
266 1 1 2 3.6 Cc1ccc2c(c1)C(c1ccccc1)=NCC(=S)N2
CHEMBL4126902 acm1_human Human No 5.4 EC50 = 3700 nM Funct
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
435 4 2 5 3.3 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(C(F)(F)F)nc2)c2ccccc2O1
CHEMBL3745962 acm1_human Human No 6.4 EC50 = 371 nM Funct
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
427 5 2 6 3.6 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-c3cncnc3)cc2)c2cccnc12
CHEMBL667 acm1_human Human Yes 6.4 EC50 = 371.5 nM Funct
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
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL1773272 acm1_rat Rat No 5.4 EC50 = 3790 nM Funct
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
487 6 1 6 4.2 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(Br)c3)c3ccccc23)no1
CHEMBL3360944 acm1_human Human No 5.4 EC50 = 3790 nM Funct
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
394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccccn4)cc-3c2=O)c(C)c1
CHEMBL4788101 acm1_human Human No 7.4 EC50 = 38 nM Funct
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
421 5 2 6 3.0 Cc1c(Cc2ccc(-c3cocn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C
CHEMBL4248057 acm1_rat Rat No 7.4 EC50 = 38.9 nM Funct
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
445 5 2 7 2.4 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cc2)n1
CHEMBL596506 acm1_human Human No 6.4 EC50 = 380 nM Bind
Positive allosteric modulation activity at muscarinic M1 receptorPositive allosteric modulation activity at muscarinic M1 receptor
373 4 1 3 4.6 O=C(O)c1cn(Cc2ccc(-c3ccccc3)cc2)c2c(F)cccc2c1=O
CHEMBL2333865 acm1_human Human Yes 5.4 EC50 = 3800 nM Bind
Positive allosteric modulation at muscarinic acetylcholine receptor M1(unknown origin)Positive allosteric modulation at muscarinic acetylcholine receptor M1(unknown origin)
390 3 0 4 3.3 CN1CCC2(C1)C(=O)N(Cc1ccc(-c3cnn(C)c3)cc1F)c1ccccc12
CHEMBL2333868 acm1_human Human No 5.4 EC50 = 3800 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
404 3 0 4 3.7 CN1CCC2(CC1)C(=O)N(Cc1ccc(-c3cnn(C)c3)cc1F)c1ccccc12
CHEMBL4127118 acm1_human Human No 5.4 EC50 = 3800 nM Funct
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
410 5 2 6 2.3 CN(C)c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1
CHEMBL2333868 acm1_human Human No 5.4 EC50 = 3801.9 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
404 3 0 4 3.7 CN1CCC2(CC1)C(=O)N(Cc1ccc(-c3cnn(C)c3)cc1F)c1ccccc12
CHEMBL4127118 acm1_human Human No 5.4 EC50 = 3801.9 nM Funct
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
410 5 2 6 2.3 CN(C)c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1
CHEMBL3360944 acm1_human Human No 5.4 EC50 = 3801.9 nM Funct
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
394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccccn4)cc-3c2=O)c(C)c1
CHEMBL965 acm1_human Human Yes 5.4 EC50 = 3811 nM Funct
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL3290087 acm1_human Human No 6.4 EC50 = 389.1 nM Bind
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
336 4 1 5 3.5 O=C(O)c1cn(Cc2ccc(N=C=S)cc2)c2ccccc2c1=O
CHEMBL1083002 acm1_human Human No 7.4 EC50 = 39.8 nM Funct
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
374 5 2 2 4.5 CC[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1
CHEMBL1083109 acm1_human Human No 7.4 EC50 = 39.8 nM Funct
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
362 4 2 2 4.4 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1Cl
CHEMBL7634 acm1_human Human Yes 6.4 EC50 = 390 nM Bind
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)
206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1
CHEMBL4097569 acm1_human Human Yes 5.4 EC50 = 3900 nM Bind
Partial agonist activity at muscarinic M1 receptor (unknown origin) assessed as recruitment of beta-arrestin by Path Hunter assayPartial agonist activity at muscarinic M1 receptor (unknown origin) assessed as recruitment of beta-arrestin by Path Hunter assay
409 5 2 6 3.0 O[C@H]1COCC[C@@H]1NC(=O)c1ncc(c(c1)Cc1ccc(cc1)c1cscn1)C
CHEMBL3618449 acm1_human Human No 6.4 EC50 = 392 nM Funct
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
449 5 2 3 4.5 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1
CHEMBL4742964 acm1_human Human No 6.4 EC50 = 392 nM Funct
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
392 5 2 6 2.0 Cc1ncc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1
CHEMBL1086479 acm1_human Human No 6.4 EC50 = 398.1 nM Funct
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
356 5 1 2 4.4 CC(=O)N(Cc1ccccc1-c1cccc(Cl)c1)CC1CCNCC1
CHEMBL1802360 acm1_human Human Yes 6.4 EC50 = 398.1 nM Funct
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
369 6 1 4 3.6 O=c1[nH]c2ccccc2n1C1CCN(CCCOc2ccc(F)cc2)CC1
CHEMBL136027 acm1_human Human No 6.4 EC50 = 398.1 nM Bind
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
495 17 0 10 5.5 COc1nsnc1OCCCCCCCCCCCCOc1nsnc1C1=CCCN(C)C1
CHEMBL2313507 acm1_human Human No 5.4 EC50 = 3981.1 nM Funct
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
387 3 1 4 3.4 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)cc2)cn1
CHEMBL4204098 acm1_human Human No 6.4 EC50 = 399 nM Funct
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
328 2 1 2 5.0 CC(C)[C@@H]1N=C(c2ccccc2)c2ccc(Cl)cc2NC1=S
CHEMBL468925 acm1_rat Rat Yes 5.4 EC50 = 3990 nM Funct
Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
333 2 0 2 3.3 O=C1C(=O)N(Cc2ccc(Br)cc2)c2c(F)cccc21
CHEMBL418491 acm1_human Human No 8.4 EC50 = 4.5 nM Funct
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.
343 3 0 5 2.6 Fc1ccc(C#CCSc2nsnc2C23CN4CC2C3C4)cc1
CHEMBL304247 acm1_human Human No 8.3 EC50 = 4.9 nM Funct
Compound was tested for its ability to stimulate phosphoinositol (PI) hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1 (100 uM concentration)Compound was tested for its ability to stimulate phosphoinositol (PI) hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1 (100 uM concentration)
327 3 0 5 1.9 Fc1cccc(C#CCOc2nsnc2C23CN4CC2C3C4)c1
CHEMBL4226420 acm1_human Human No 7.4 EC50 = 40 nM Funct
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
436 6 3 7 1.7 Cn1c(CO)c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c1=O
CHEMBL4240041 acm1_rat Rat No 7.4 EC50 = 40 nM Funct
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
444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1
CHEMBL4248057 acm1_rat Rat No 7.4 EC50 = 40 nM Funct
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
445 5 2 7 2.4 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cc2)n1
CHEMBL1802360 acm1_human Human Yes 6.4 EC50 = 400 nM Funct
Agonist activity at human M1 muscarinic receptor expressed in CHO cells assessed as inhibition of carbachol-stimulated phosphatidyl-inositol hydrolysis by cell-based functional assayAgonist activity at human M1 muscarinic receptor expressed in CHO cells assessed as inhibition of carbachol-stimulated phosphatidyl-inositol hydrolysis by cell-based functional assay
369 6 1 4 3.6 O=c1[nH]c2ccccc2n1C1CCN(CCCOc2ccc(F)cc2)CC1
CHEMBL2059304 acm1_human Human Yes 6.4 EC50 = 400 nM Funct
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
337 5 1 4 3.0 O=c1[nH]c2ccccc2n1C1CCN(CCOc2ccccc2)CC1
CHEMBL978 acm1_rat Rat Yes 6.4 EC50 = 400 nM Funct
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C
CHEMBL2313507 acm1_human Human No 5.4 EC50 = 4000 nM Funct
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
387 3 1 4 3.4 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)cc2)cn1
CHEMBL965 acm1_mouse Mouse Yes 4.4 EC50 = 40000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL4745001 acm1_human Human No 6.4 EC50 = 405 nM Funct
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
400 6 2 5 3.5 CC(C)(O)CNC(=O)c1cc(Cc2ccc(-c3ccncc3)cc2)c2cccn2n1
CHEMBL2333480 acm1_human Human No 5.4 EC50 = 4073.8 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
462 4 0 4 4.8 Cn1cc(-c2cc(F)c(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)cc2F)cn1
CHEMBL2333483 acm1_human Human No 5.4 EC50 = 4073.8 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
422 5 0 4 3.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(CCF)C4)c4ccccc43)c(F)c2)cn1
CHEMBL2022960 acm1_human Human Yes 7.4 EC50 = 41 nM Funct
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F
CHEMBL2063422 acm1_human Human No 7.4 EC50 = 41 nM Bind
Positive allosteric modulation activity at muscarinic M1 receptorPositive allosteric modulation activity at muscarinic M1 receptor
395 4 1 5 3.4 Cn1cc(-c2ccc(Cn3cc(C(=O)O)c(=O)c4c(F)cccc43)c(F)c2)cn1
CHEMBL4747042 acm1_human Human No 7.4 EC50 = 41 nM Funct
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
440 5 2 5 4.3 Cc1cccc(-c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)nn4cccc34)cc2)n1
CHEMBL3354068 acm1_human Human No 7.4 EC50 = 41.7 nM Bind
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
565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1
CHEMBL4240041 acm1_rat Rat No 7.4 EC50 = 41.7 nM Funct
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
444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1
CHEMBL478662 acm1_human Human No 6.4 EC50 = 410 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
458 4 1 4 4.7 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1
CHEMBL2024326 acm1_human Human No 5.4 EC50 = 4100 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
331 6 2 4 1.4 CCOC(=O)N1C[C@H]2C(NCCNC(=O)c3ccccc3C)[C@H]2C1
CHEMBL521030 acm1_human Human No 5.4 EC50 = 4100 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
474 4 1 5 3.5 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1
CHEMBL2333480 acm1_human Human No 5.4 EC50 = 4100 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
462 4 0 4 4.8 Cn1cc(-c2cc(F)c(CN3C(=O)C4(CCN(C5CCCC5)C4)c4ccccc43)cc2F)cn1
CHEMBL2333483 acm1_human Human No 5.4 EC50 = 4100 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
422 5 0 4 3.7 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(CCF)C4)c4ccccc43)c(F)c2)cn1
CHEMBL1194965 acm1_mouse Mouse Yes 4.4 EC50 = 41000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1
CHEMBL553602 acm1_mouse Mouse Yes 4.4 EC50 = 41000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1
CHEMBL4213762 acm1_human Human No 6.4 EC50 = 414 nM Funct
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
334 2 1 2 5.5 CC(C)[C@@H]1N=C(C2CCCCC2)c2cc(Cl)ccc2NC1=S
CHEMBL3290085 acm1_human Human No 6.4 EC50 = 416.9 nM Bind
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
374 4 1 5 2.2 O=C(O)c1cn(Cc2ccc(N3C(=O)C=CC3=O)cc2)c2ccccc2c1=O
CHEMBL4203058 acm1_human Human No 6.4 EC50 = 420 nM Funct
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
346 2 1 2 5.1 CC(C)[C@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S
CHEMBL3616497 acm1_human Human No 6.4 EC50 = 426 nM Funct
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
521 7 3 4 4.7 COc1ccc(CCN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1
CHEMBL3823474 acm1_rat Rat No 5.4 EC50 = 4265.8 nM Funct
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
404 3 0 4 4.1 Cn1cc2c(-c3cc(F)c(CN4CCc5ncccc5C4=O)c(F)c3)cccc2n1
CHEMBL337925 acm1_human Human No 6.4 EC50 = 430.9 nM Funct
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.
285 5 0 6 2.5 CCCSc1nsnc1OC1CN2CCC1CC2
CHEMBL3823474 acm1_rat Rat No 5.4 EC50 = 4300 nM Funct
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
404 3 0 4 4.1 Cn1cc2c(-c3cc(F)c(CN4CCc5ncccc5C4=O)c(F)c3)cccc2n1
CHEMBL125732 acm1_human Human Yes 6.4 EC50 = 433.3 nM Funct
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.
313 7 0 6 3.3 CCCCCSc1nsnc1OC1CN2CCC1CC2
CHEMBL2059322 acm1_human Human No 7.4 EC50 = 44 nM Funct
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
424 5 1 5 2.9 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3ccc(F)cc32)CC1
CHEMBL2024421 acm1_human Human No 6.4 EC50 = 440 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
379 6 2 4 2.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cccc(Cl)c1)C2
CHEMBL343055 acm1_human Human No 6.4 EC50 = 440 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
452 7 0 10 3.7 CN1CCC=C(c2nsnc2SCCSc2nsnc2C2=CCCN(C)C2)C1
CHEMBL487984 acm1_human Human No 5.4 EC50 = 4400 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
518 4 1 5 3.6 O=c1[nH]c2cc(Br)ccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1
CHEMBL1773114 acm1_rat Rat No 5.4 EC50 = 4400 nM Funct
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
493 7 2 7 3.9 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cn[nH]c4)c3F)c3ccccc23)no1
CHEMBL1190710 acm1_mouse Mouse Yes 4.4 EC50 = 44000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1
CHEMBL541398 acm1_mouse Mouse Yes 4.4 EC50 = 44000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1
CHEMBL20835 acm1_human Human Yes 5.4 EC50 = 4466 nM Funct
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.
169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2
CHEMBL4097569 acm1_human Human Yes 6.4 EC50 = 447 nM Funct
Positive allosteric modulation of muscarinic M1 receptor (unknown origin) expressed in CHO cells assessed as increase in Ach-induced accumulation of inositol phosphate accumulation measured after 30 mins by HTRF assayPositive allosteric modulation of muscarinic M1 receptor (unknown origin) expressed in CHO cells assessed as increase in Ach-induced accumulation of inositol phosphate accumulation measured after 30 mins by HTRF assay
409 5 2 6 3.0 O[C@H]1COCC[C@@H]1NC(=O)c1ncc(c(c1)Cc1ccc(cc1)c1cscn1)C
CHEMBL4211633 acm1_human Human Yes 5.4 EC50 = 4479 nM Funct
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
297 2 1 4 3.2 O=[N+]([O-])c1ccc2c(c1)C(c1ccccc1)=NCC(=S)N2
CHEMBL4096607 acm1_human Human No 7.4 EC50 = 45 nM Funct
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
417 4 1 5 3.2 Cc1cn(-c2ccc(Cc3cc4c(cc3C)CN([C@H]3CCOC[C@@H]3O)C4=O)cc2)cn1
CHEMBL1242950 acm1_human Human Yes 6.4 EC50 = 450 nM Funct
Partial agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayPartial agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C
CHEMBL3746322 acm1_human Human No 5.4 EC50 = 4500 nM Funct
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
415 5 2 6 3.3 O=C(N[C@H]1CCCC[C@@H]1O)c1nn(Cc2ccc(-n3cccn3)cc2)c2ccccc12
CHEMBL1243233 acm1_human Human No 7.3 EC50 = 46 nM Funct
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
359 6 1 4 2.0 CC(C)C(=O)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1
CHEMBL60331 acm1_human Human No 7.3 EC50 = 46 nM Funct
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.
377 3 0 5 3.3 Fc1cc(Cl)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1
CHEMBL667 acm1_human Human Yes 7.3 EC50 = 46.8 nM Bind
Agonist activity at recombinant human muscarinic M1 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M1 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL304142 acm1_human Human Yes 6.3 EC50 = 460 nM Bind
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)
168 1 1 4 0.7 COc1noc2c1CNCCC2
CHEMBL965 acm1_human Human Yes 5.3 EC50 = 4600 nM Bind
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)
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL965 acm1_human Human Yes 5.3 EC50 = 4600 nM Funct
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.
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL3084449 acm1_human Human No 7.3 EC50 = 47 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
379 6 2 4 2.5 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccc(Cl)c1
CHEMBL667 acm1_human Human Yes 7.3 EC50 = 47 nM Bind
Agonist activity at recombinant human muscarinic M1 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M1 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL4067722 acm1_human Human Yes 7.3 EC50 = 47 nM Funct
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
404 4 1 5 3.3 Cc1cc2c(cc1Cc1ccc(-c3cocn3)cc1)C(=O)N([C@H]1CCOC[C@@H]1O)C2
CHEMBL3608416 acm1_human Human No 7.3 EC50 = 47.9 nM Funct
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
463 5 2 7 2.9 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@]4(C)O)c4ncccc43)c(F)c2)cn1
CHEMBL2024324 acm1_human Human No 6.3 EC50 = 470 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
377 6 2 4 2.6 CCOC(=O)N1[C@H]2CC[C@@H]1CC(NCCNC(=O)c1ccc(C)c(F)c1)C2
CHEMBL313918 acm1_human Human No 5.3 EC50 = 4700 nM Funct
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
202 2 0 3 0.7 C#CCC#CCO/N=C1\CN2CCC1C2
CHEMBL3822763 acm1_rat Rat No 5.3 EC50 = 4700 nM Funct
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
402 3 0 5 4.3 Cn1cc2c(-c3cc(F)c(Cn4cnc5ccccc5c4=O)c(F)c3)cccc2n1
CHEMBL3823885 acm1_rat Rat No 5.3 EC50 = 4700 nM Funct
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
403 3 0 6 3.7 Cn1cc2c(-c3cc(F)c(Cn4cnc5cnccc5c4=O)c(F)c3)cccc2n1
CHEMBL1556989 acm1_human Human Yes 6.3 EC50 = 473 nM Funct
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
393 4 0 4 5.0 Cc1ccc(C)c(Cn2nc3c4ccccc4n(Cc4ccccc4)cc-3c2=O)c1
CHEMBL3745995 acm1_human Human No 6.3 EC50 = 478 nM Funct
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
374 4 2 5 3.0 N#Cc1ccc(Cn2cc(C(=O)N[C@H]3CCCC[C@@H]3O)c3ncccc32)cc1
CHEMBL4130009 acm1_human Human No 6.3 EC50 = 478.6 nM Funct
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
432 5 2 6 3.1 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccc3)nc2)c2ccccc2O1
CHEMBL4116342 acm1_human Human No 5.3 EC50 = 4786.3 nM Bind
Agonist activity at Gq/11 coupled recombinant human muscarinic M1 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M1 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
206 3 0 1 1.9 C[N+](C)(C)CCC1=CC2=C(CCO2)C=C1
CHEMBL3822763 acm1_rat Rat No 5.3 EC50 = 4786.3 nM Funct
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
402 3 0 5 4.3 Cn1cc2c(-c3cc(F)c(Cn4cnc5ccccc5c4=O)c(F)c3)cccc2n1
CHEMBL3823885 acm1_rat Rat No 5.3 EC50 = 4786.3 nM Funct
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
403 3 0 6 3.7 Cn1cc2c(-c3cc(F)c(Cn4cnc5cnccc5c4=O)c(F)c3)cccc2n1
CHEMBL2313498 acm1_human Human No 5.3 EC50 = 4786.3 nM Funct
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
405 3 1 4 3.5 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1
CHEMBL1243110 acm1_human Human No 7.3 EC50 = 48 nM Funct
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
405 7 1 3 3.2 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3ccccc32)CC1
CHEMBL3618444 acm1_human Human No 7.3 EC50 = 48.4 nM Funct
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
495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1cccc(F)c1
CHEMBL4116342 acm1_human Human No 5.3 EC50 = 4800 nM Bind
Agonist activity at Gq/11 coupled recombinant human muscarinic M1 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assayAgonist activity at Gq/11 coupled recombinant human muscarinic M1 AChR expressed in CHO-FlpIn cells assessed as IP-one accumulation after 40 mins by HTRF assay
206 3 0 1 1.9 C[N+](C)(C)CCC1=CC2=C(CCO2)C=C1
CHEMBL4229203 acm1_human Human Yes 5.3 EC50 = 4800 nM Funct
Allosteric agonist at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as induction of calcium mobilization after 2.5 mins by Fluo-4AM-based FLIPR assayAllosteric agonist at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as induction of calcium mobilization after 2.5 mins by Fluo-4AM-based FLIPR assay
465 5 2 6 3.8 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@@H]4CCCC[C@H]4O)c4c(F)cc(F)cc43)cn2)cn1
CHEMBL2313498 acm1_human Human No 5.3 EC50 = 4800 nM Funct
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
405 3 1 4 3.5 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1
CHEMBL129474 acm1_human Human No 5.3 EC50 = 4867 nM Funct
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.
243 6 1 6 1.5 CCCCOc1nsnc1OC1CCNC1
CHEMBL4241339 acm1_rat Rat No 6.3 EC50 = 489.8 nM Funct
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
430 6 1 7 2.9 Cn1ccc(-c2ccc(Cc3cc(C(=O)NC[C@@H]4CCCO4)nc4c3ccn4C)cn2)n1
CHEMBL4243017 acm1_rat Rat No 6.3 EC50 = 489.8 nM Funct
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
415 5 1 6 3.3 Cn1ccc2c(Cc3ccc(-n4cccn4)cc3)cc(C(=O)NC3CCOCC3)nc21
CHEMBL3823059 acm1_rat Rat No 5.3 EC50 = 4897.8 nM Funct
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
402 3 0 5 4.3 Cn1cc2c(-c3cc(F)c(Cn4c(=O)cnc5ccccc54)c(F)c3)cccc2n1
CHEMBL1243043 acm1_human Human No 7.3 EC50 = 49 nM Funct
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
423 7 1 3 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3cc(F)ccc32)CC1
CHEMBL3616499 acm1_human Human No 7.3 EC50 = 49.5 nM Funct
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
445 5 2 3 4.7 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1
CHEMBL476990 acm1_human Human No 6.3 EC50 = 490 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
415 4 1 5 3.5 N#Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1
CHEMBL4241339 acm1_rat Rat No 6.3 EC50 = 490 nM Funct
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
430 6 1 7 2.9 Cn1ccc(-c2ccc(Cc3cc(C(=O)NC[C@@H]4CCCO4)nc4c3ccn4C)cn2)n1
CHEMBL4243017 acm1_rat Rat No 6.3 EC50 = 490 nM Funct
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
415 5 1 6 3.3 Cn1ccc2c(Cc3ccc(-n4cccn4)cc3)cc(C(=O)NC3CCOCC3)nc21
CHEMBL3823059 acm1_rat Rat No 5.3 EC50 = 4900 nM Funct
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
402 3 0 5 4.3 Cn1cc2c(-c3cc(F)c(Cn4c(=O)cnc5ccccc54)c(F)c3)cccc2n1
CHEMBL1223753 acm1_human Human Yes 8.3 EC50 = 5.0 nM Funct
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
333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1
CHEMBL2146599 acm1_human Human Yes 8.3 EC50 = 5.0 nM Funct
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
315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1
CHEMBL4063980 acm1_human Human No 7.3 EC50 = 50 nM Funct
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
418 4 1 5 3.7 Cc1nc(-c2ccc(Cc3cc4c(cc3C)CN([C@H]3CCOC[C@@H]3O)C4=O)cc2)co1
CHEMBL4212168 acm1_human Human No 7.3 EC50 = 50 nM Funct
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
316 2 1 2 5.3 CCC1CN(c2ccccc2)c2cc(Cl)ccc2NC1=S
CHEMBL335542 acm1_human Human No 7.3 EC50 = 50.1 nM Funct
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
552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1
CHEMBL1082679 acm1_human Human No 7.3 EC50 = 50.1 nM Funct
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
346 4 2 2 3.9 O=C(NCC1CCNCC1)c1cc(F)ccc1-c1cccc(Cl)c1
CHEMBL1084805 acm1_human Human No 7.3 EC50 = 50.1 nM Funct
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
342 4 1 2 3.8 CN(C(=O)Cc1ccccc1-c1cccc(Cl)c1)C1CCNCC1
CHEMBL1084819 acm1_human Human No 7.3 EC50 = 50.1 nM Funct
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
362 4 2 2 4.4 O=C(NCC1CCNCC1)c1ccccc1-c1ccc(Cl)c(Cl)c1
CHEMBL1242950 acm1_human Human Yes 6.3 EC50 = 500 nM Funct
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
301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C
CHEMBL3747287 acm1_human Human No 6.3 EC50 = 500 nM Funct
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
401 6 2 6 2.9 O=C(NCC1(O)CCC1)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12
CHEMBL4130009 acm1_human Human No 6.3 EC50 = 500 nM Funct
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
432 5 2 6 3.1 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccc3)nc2)c2ccccc2O1
CHEMBL1916235 acm1_rat Rat No 5.3 EC50 = 5000 nM Funct
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
351 4 1 4 2.4 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)C3CCCC3)C2)CC1
CHEMBL2333863 acm1_human Human No 5.3 EC50 = 5000 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
486 4 0 4 4.8 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C(=O)C5CCCCC5)C4)c4ccccc43)c(F)c2)cn1
CHEMBL1191028 acm1_mouse Mouse Yes 4.3 EC50 = 50000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
180 2 1 4 -0.2 CC#CCOC(=O)C1CN=CNC1
CHEMBL542064 acm1_mouse Mouse Yes 4.3 EC50 = 50000 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
180 2 1 4 -0.2 CC#CCOC(=O)C1CN=CNC1
CHEMBL219118 acm1_human Human No 6.3 EC50 = 501.2 nM Funct
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
467 16 0 12 3.1 COc1nsc(OCCCOCCCOCCCOc2nsnc2-c2cccnc2)n1
CHEMBL1083403 acm1_human Human No 6.3 EC50 = 501.2 nM Funct
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
391 3 1 4 5.3 Fc1cccc(-c2cc(Cl)ccc2Cl)c1-c1nc(C2CCNCC2)no1
CHEMBL1085556 acm1_human Human No 6.3 EC50 = 501.2 nM Funct
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
328 4 2 2 3.6 O=C(NCc1ccccc1-c1cccc(Cl)c1)C1CCNCC1
CHEMBL965 acm1_human Human Yes 5.3 EC50 = 5011.9 nM Funct
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
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL1082362 acm1_human Human No 5.3 EC50 = 5011.9 nM Funct
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
346 4 2 2 3.9 O=C(NCC1CCNCC1)c1cccc(F)c1-c1cccc(Cl)c1
CHEMBL2333863 acm1_human Human No 5.3 EC50 = 5011.9 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
486 4 0 4 4.8 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C(=O)C5CCCCC5)C4)c4ccccc43)c(F)c2)cn1
CHEMBL168561 acm1_human Human No 5.3 EC50 = 5050 nM Funct
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
216 2 0 3 1.1 CC#CCC#CCO/N=C1\CN2CCC1C2
CHEMBL3618436 acm1_human Human No 7.3 EC50 = 51 nM Funct
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
481 4 3 3 5.1 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)Nc1ccc(F)cc1
CHEMBL1243044 acm1_human Human No 7.3 EC50 = 51 nM Funct
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
423 7 1 3 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3ccc(F)cc32)CC1
CHEMBL3608417 acm1_rat Rat No 7.3 EC50 = 51 nM Funct
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
449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)c(F)c2)cn1
CHEMBL513765 acm1_human Human No 6.3 EC50 = 510 nM Funct
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
418 3 1 4 3.6 Cc1cccc(C(=O)N2CCC(N3CCC(n4c(=O)[nH]c5ccccc54)CC3)CC2)c1
CHEMBL1773112 acm1_rat Rat No 5.3 EC50 = 5100 nM Funct
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
461 6 1 6 4.2 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(Cl)c3F)c3ccccc23)no1
CHEMBL83074 acm1_human Human No 5.3 EC50 = 5100 nM Funct
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
240 2 0 3 1.1 C#CCC#CCC#CCO/N=C1\CN2CCC1C2
CHEMBL4227175 acm1_human Human No 6.3 EC50 = 511 nM Funct
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
408 5 3 7 1.4 Cc1cnc(C(=O)N[C@H]2CCOC(O)[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1
CHEMBL2333872 acm1_human Human No 5.3 EC50 = 5128.6 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
458 4 0 4 5.0 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCCC5)C4)c4ccccc43)c(F)c2)cn1
CHEMBL2313512 acm1_human Human No 5.3 EC50 = 5128.6 nM Funct
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
337 3 0 4 3.2 Cn1cc(-c2ccc(CN3C(=O)COc4ccccc43)c(F)c2)cn1
CHEMBL4218606 acm1_human Human Yes 6.3 EC50 = 516 nM Funct
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
320 1 1 2 4.3 FC(F)(F)c1ccc2c(c1)C(c1ccccc1)=NCC(=S)N2
CHEMBL468290 acm1_rat Rat No 5.3 EC50 = 5180 nM Funct
Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
323 2 0 2 3.6 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(F)cccc21
CHEMBL2333872 acm1_human Human No 5.3 EC50 = 5200 nM Bind
Positive allosteric modulation of human muscarinic M1 receptorPositive allosteric modulation of human muscarinic M1 receptor
458 4 0 4 5.0 Cn1cc(-c2ccc(CN3C(=O)C4(CCN(C5CCCCC5)C4)c4ccccc43)c(F)c2)cn1
CHEMBL2313512 acm1_human Human No 5.3 EC50 = 5200 nM Funct
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
337 3 0 4 3.2 Cn1cc(-c2ccc(CN3C(=O)COc4ccccc43)c(F)c2)cn1
CHEMBL4216528 acm1_human Human No 6.3 EC50 = 521 nM Funct
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
328 2 1 2 5.0 CC(C)[C@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S
CHEMBL1300017 acm1_rat Rat Yes 5.3 EC50 = 5220 nM Funct
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
427 6 1 6 3.5 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(F)c3)c3ccccc23)no1
CHEMBL3824092 acm1_rat Rat No 5.3 EC50 = 5248.1 nM Funct
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
403 3 0 6 3.7 Cn1cnc2ccc(-c3cc(F)c(Cn4cnc5cnccc5c4=O)c(F)c3)cc21
CHEMBL1255785 acm1_human Human Yes 5.3 EC50 = 5300 nM Bind
Activation of M1-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M1-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O
CHEMBL12587 acm1_human Human Yes 5.3 EC50 = 5300 nM Bind
Activation of M1-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M1-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O
CHEMBL292911 acm1_human Human Yes 5.3 EC50 = 5300 nM Bind
Activation of M1-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M1-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O
CHEMBL3823885 acm1_human Human No 5.3 EC50 = 5300 nM Funct
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
403 3 0 6 3.7 Cn1cc2c(-c3cc(F)c(Cn4cnc5cnccc5c4=O)c(F)c3)cccc2n1
CHEMBL3824092 acm1_rat Rat No 5.3 EC50 = 5300 nM Funct
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
403 3 0 6 3.7 Cn1cnc2ccc(-c3cc(F)c(Cn4cnc5cnccc5c4=O)c(F)c3)cc21
CHEMBL1300017 acm1_rat Rat Yes 5.3 EC50 = 5324 nM Funct
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])]
427 6 1 6 3.5 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(F)c3)c3ccccc23)no1
CHEMBL4115997 acm1_human Human Yes 6.3 EC50 = 537.0 nM Bind
Agonist activity at recombinant human muscarinic M1 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M1 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
194 4 0 1 1.9 C[N+](C)(C)CCC1=CC(=CC=C1)OC
CHEMBL3414845 acm1_human Human No 6.3 EC50 = 537.0 nM Funct
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
329 8 1 3 4.3 CCCCCCCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1
CHEMBL1773110 acm1_rat Rat No 5.3 EC50 = 5370 nM Funct
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
523 6 1 6 4.4 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(Br)c3)c3cc(F)cc(F)c23)no1
CHEMBL511254 acm1_rat Rat Yes 5.3 EC50 = 5380 nM Funct
Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
301 3 0 3 3.1 COc1ccc(CN2C(=O)C(=O)c3cccc(Cl)c32)cc1
CHEMBL4115997 acm1_human Human Yes 6.3 EC50 = 540 nM Bind
Agonist activity at recombinant human muscarinic M1 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at recombinant human muscarinic M1 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
194 4 0 1 1.9 C[N+](C)(C)CCC1=CC(=CC=C1)OC
CHEMBL3329755 acm1_human Human Yes 5.3 EC50 = 5400 nM Funct
Activity at human muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assayActivity at human muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assay
494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F
CHEMBL2024412 acm1_human Human No 5.3 EC50 = 5400 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
343 6 2 3 2.2 CC(C)C(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1)C2
CHEMBL1183042 acm1_mouse Mouse Yes 5.3 EC50 = 5400 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1
CHEMBL277014 acm1_mouse Mouse Yes 5.3 EC50 = 5400 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1
CHEMBL4238850 acm1_rat Rat No 6.3 EC50 = 549.5 nM Funct
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
458 5 1 7 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)NC4CCOC(C)(C)C4)nc4c3ccn4C)cn2)n1
CHEMBL3747016 acm1_human Human Yes 7.3 EC50 = 55 nM Funct
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
431 5 2 7 2.4 Cn1ccc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@H]4O)c4ncccc43)cc2)n1
CHEMBL3747016 acm1_human Human Yes 7.3 EC50 = 55 nM Funct
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
431 5 2 7 2.4 Cn1ccc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@H]4O)c4ncccc43)cc2)n1
CHEMBL3747016 acm1_human Human Yes 7.3 EC50 = 55 nM Funct
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
431 5 2 7 2.4 Cn1ccc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@H]4O)c4ncccc43)cc2)n1
CHEMBL4238850 acm1_rat Rat No 6.3 EC50 = 550 nM Funct
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
458 5 1 7 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)NC4CCOC(C)(C)C4)nc4c3ccn4C)cn2)n1
CHEMBL4210331 acm1_human Human No 6.3 EC50 = 552 nM Funct
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
266 1 1 2 3.7 CC1N=C(c2ccccc2)c2ccccc2NC1=S
CHEMBL4205971 acm1_human Human No 6.3 EC50 = 559 nM Funct
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
324 3 1 3 4.3 COc1ccc2c(c1)C(c1ccccc1)=N[C@@H](C(C)C)C(=S)N2
CHEMBL1243075 acm1_human Human No 6.3 EC50 = 560 nM Funct
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
435 8 1 4 3.2 COc1ccc2c(c1)CCC(=O)N2CCCN1CCC(NC(=O)Cc2ccccc2)CC1
CHEMBL4248900 acm1_rat Rat No 6.3 EC50 = 560 nM Funct
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
429 5 1 6 3.5 Cn1ccc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cc2)n1
CHEMBL2313508 acm1_human Human No 5.3 EC50 = 5600 nM Funct
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
335 3 0 3 3.7 Cn1cc(-c2ccc(CN3C(=O)CCc4ccccc43)c(F)c2)cn1
CHEMBL7303 acm1_human Human Yes 5.3 EC50 = 5603 nM Funct
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C
CHEMBL4248900 acm1_rat Rat No 6.3 EC50 = 562.3 nM Funct
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
429 5 1 6 3.5 Cn1ccc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cc2)n1
CHEMBL4237601 acm1_rat Rat No 5.3 EC50 = 5620 nM Funct
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
448 5 2 7 3.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)N[C@@H]3CCOC[C@H]3O)nc21
CHEMBL4237601 acm1_rat Rat No 5.3 EC50 = 5623.4 nM Funct
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
448 5 2 7 3.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)N[C@@H]3CCOC[C@H]3O)nc21
CHEMBL2313508 acm1_human Human No 5.3 EC50 = 5623.4 nM Funct
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
335 3 0 3 3.7 Cn1cc(-c2ccc(CN3C(=O)CCc4ccccc43)c(F)c2)cn1
CHEMBL3402918 acm1_human Human No 5.3 EC50 = 5680 nM Funct
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
226 3 0 4 1.8 CSCC1CC(C2=CCCN(C)C2)=NO1
CHEMBL965 acm1_human Human Yes 5.3 EC50 = 5690 nM Funct
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
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL21536 acm1_human Human Yes 7.2 EC50 = 57 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL3414838 acm1_human Human No 7.2 EC50 = 57.5 nM Funct
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
533 10 1 6 3.5 C[N+](C)(CC#CCOC1=NOCC1)CCCCNC(=O)c1cn(Cc2ccccc2)c2c(F)cccc2c1=O
CHEMBL3559073 acm1_human Human No 7.2 EC50 = 57.5 nM Funct
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
533 10 1 6 3.5 C[N+](C)(CC#CCOC1=NOCC1)CCCCNC(=O)c1cn(Cc2ccccc2)c2c(F)cccc2c1=O
CHEMBL2022942 acm1_human Human No 6.2 EC50 = 570 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
352 5 2 4 1.9 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)N1CCCCC1)C2
CHEMBL142184 acm1_human Human No 6.2 EC50 = 570 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
480 9 0 10 4.5 CN1CCC=C(c2nsnc2SCCCCSc2nsnc2C2=CCCN(C)C2)C1
CHEMBL4245109 acm1_rat Rat No 6.2 EC50 = 570 nM Funct
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
442 5 1 7 2.9 Cn1ccc(-c2ccc(Cc3cc(C(=O)NC4CC5(COC5)C4)nc4c3ccn4C)cn2)n1
CHEMBL21536 acm1_mouse Mouse Yes 5.2 EC50 = 5700 nM Bind
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL3618442 acm1_human Human No 6.2 EC50 = 572 nM Funct
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
507 6 3 4 4.7 COc1ccccc1CN/C(C)=N/c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2
CHEMBL4247625 acm1_rat Rat No 6.2 EC50 = 575 nM Funct
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
446 5 2 8 1.8 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cn2)n1
CHEMBL4247625 acm1_rat Rat No 6.2 EC50 = 575.4 nM Funct
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
446 5 2 8 1.8 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cn2)n1
CHEMBL4245109 acm1_rat Rat No 6.2 EC50 = 575.4 nM Funct
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
442 5 1 7 2.9 Cn1ccc(-c2ccc(Cc3cc(C(=O)NC4CC5(COC5)C4)nc4c3ccn4C)cn2)n1
CHEMBL3608414 acm1_rat Rat No 7.2 EC50 = 58.6 nM Funct
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
449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@H]4O)c4ncccc43)c(F)c2)cn1
CHEMBL3414844 acm1_human Human No 7.2 EC50 = 58.9 nM Funct
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
561 12 1 6 4.3 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2ccc(F)cc2c1=O
CHEMBL3559052 acm1_human Human No 7.2 EC50 = 58.9 nM Funct
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
561 12 1 6 4.3 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2ccc(F)cc2c1=O
CHEMBL1438248 acm1_rat Rat No 5.2 EC50 = 5820 nM Funct
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
443 6 1 6 4.1 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(Cl)c3)c3ccccc23)no1
CHEMBL1438248 acm1_rat Rat No 5.2 EC50 = 5857 nM Funct
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])]
443 6 1 6 4.1 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(Cl)c3)c3ccccc23)no1
CHEMBL511206 acm1_rat Rat Yes 5.2 EC50 = 5880 nM Funct
Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
305 2 0 2 3.4 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccccc21
CHEMBL4128118 acm1_human Human No 5.2 EC50 = 5888.4 nM Funct
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
406 6 2 6 2.5 CC(C)(O)CNC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1
CHEMBL2024331 acm1_human Human No 7.2 EC50 = 59 nM Funct
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3C)C1)C2
CHEMBL341759 acm1_human Human No 6.2 EC50 = 590 nM Funct
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
508 11 0 10 5.3 CN1CCC=C(c2nsnc2SCCCCCCSc2nsnc2C2=CCCN(C)C2)C1
CHEMBL168545